Explore a selection of our essential drug information below, or:
Identification
- Summary
Procaine is a local anesthetic used for anesthesia, peripheral nerve block, and spinal nerve block.
- Brand Names
- Novocain
- Generic Name
- Procaine
- DrugBank Accession Number
- DB00721
- Background
A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). Procaine has also been investigated as an oral entry inhibitor in treatment-experienced HIV patients 2.
- Type
- Small Molecule
- Groups
- Approved, Investigational, Vet approved
- Structure
Structure for Procaine (DB00721)
- Weight
- Average: 236.3101
Monoisotopic: 236.152477894 - Chemical Formula
- C13H20N2O2
- Synonyms
- 2-Diethylaminoethyl p-aminobenzoate
- 4-aminobenzoic acid 2-diethylaminoethyl ester
- Novocaine
- p-Aminobenzoic acid 2-diethylaminoethyl ester
- Procaina
- Procaine
- Procainum
- Vitamin H3
- β-(diethylamino)ethyl 4-aminobenzoate
- β-(diethylamino)ethyl p-aminobenzoate
Pharmacology
- Indication
Used as a local anesthetic primarily in oral surgery
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Otalgia Combination Product in combination with: Antipyrine (DB01435) •••••••••••• •••••••• • ••••• - Contraindications & Blackbox Warnings
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Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine.
- Mechanism of action
Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Target Actions Organism ASodium channel protein type 10 subunit alpha inhibitorHumans AGlutamate receptor ionotropic, NMDA 3A antagonistHumans A5-hydroxytryptamine receptor 3A antagonistHumans ASodium-dependent dopamine transporter inhibitorHumans UNeuronal acetylcholine receptor subunit alpha-2 antagonistHumans UCalcium-activated potassium channel blockerHumans UCytosolic phospholipase A2 inhibitorHumans U60 kDa lysophospholipase inhibitorHumans UMonoamine oxidase inhibitorHumans UDNA (cytosine-5)-methyltransferase 1 inhibitorHumans UDNA (cytosine-5)-methyltransferase 3A inhibitorHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Hydrolysis by plasma esterases to PABA
Hover over products below to view reaction partners
- Route of elimination
With normal kidney function, the drug is excreted rapidly by tubular excretion.
- Half-life
7.7 minutes
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
Pathway Category Procaine Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Procaine is combined with 1,2-Benzodiazepine. Abaloparatide Procaine may increase the orthostatic hypotensive activities of Abaloparatide. Abciximab The risk or severity of bleeding and hemorrhage can be increased when Procaine is combined with Abciximab. Abemaciclib The risk or severity of methemoglobinemia can be increased when Abemaciclib is combined with Procaine. Abiraterone The risk or severity of methemoglobinemia can be increased when Abiraterone is combined with Procaine. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Procaine hydrochloride 95URV01IDQ 51-05-8 HCBIBCJNVBAKAB-UHFFFAOYSA-N Procaine nitrate T824SI1PU1 6192-92-3 XUXYDJABBYUMRY-UHFFFAOYSA-N Procaine phosphate A18LHT9ZXJ 54812-66-7 NPBISBZNYVWJOL-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Novocain Injection, solution 10 mg/1mL Infiltration Hospira, Inc. 2007-04-16 Not applicable US 
Novocain Injection, solution 20 mg/1mL Infiltration Hospira, Inc. 2007-04-16 Not applicable US Novocain Injection, solution 10 mg/1mL Infiltration Hospira, Inc. 2007-04-16 Not applicable US Novocain 20 mg/ml Solution 2 % Infiltration Hospira Healthcare Ulc 2001-06-01 2012-08-03 Canada 
Novocain Liq 2% Liquid 2 % Infiltration Sanofi S.R.L. 1920-12-31 2001-08-10 Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image PROCANOL LOTION 2% Lotion 2 % Topical ICM PHARMA PTE. LTD. 1997-01-25 Not applicable Singapore 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image DBL STERILE CARDIOPLEGIA CONCENTRATE Procaine hydrochloride (1 mmol/20ml) + Magnesium chloride (16 mmol/20ml) + Potassium chloride (16 mmol/20ml) Injection Other Hospira, Inc. 1988-06-16 Not applicable Singapore DBL STERILE CARDIOPLEGIA CONCENTRATE Procaine hydrochloride (13.6 mg/ml) + Magnesium chloride (162.7 mg/ml) + Potassium chloride (59.6 mg/ml) Injection Other Tempo Scan Pacific Tbk 2018-12-04 2023-12-04 Indonesia 
DBL STERILE CARDIOPLEGIA CONCENTRATE Procaine hydrochloride (1 mmol/20mL) + Magnesium chloride hexahydrate (16 mmol/20mL) + Potassium chloride (16 mmol/20mL) Injection, solution, concentrate Intravenous บริษัท ไฟเซอร์ (ประเทศไทย) จำกัด 2019-07-09 Not applicable Thailand 
Sterile Concentrate For Cardioplegia Infusion Procaine hydrochloride (14 mg/ml) + Magnesium chloride hexahydrate (163 mg/ml) + Potassium chloride (60 mg/ml) Concentrate Intravenous drip IMEKS PHARMA SDN. BHD. 2020-09-08 2020-12-17 Malaysia 
Categories
- ATC Codes
- N01BA52 — Procaine, combinationsC05AD05 — Procaine
- C05AD — Local anesthetics
- C05A — AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Acids, Carbocyclic
- Agents for Treatment of Hemorrhoids and Anal Fissures for Topical Use
- Agents that reduce seizure threshold
- Aminobenzoates
- Anesthetics
- Anesthetics, Local
- Anticholinergic Agents
- Antidepressive Agents
- Benzene Derivatives
- Benzoates
- Central Nervous System Agents
- Central Nervous System Depressants
- Cholinesterase Inhibitors
- Cholinesterase substrates
- Esters of Aminobenzoic Acid
- Local Anesthetics (Ester)
- Methemoglobinemia Associated Agents
- Monoamine Oxidase Inhibitors
- Nervous System
- Nicotinic Antagonists
- NMDA Receptor Antagonists
- Ophthalmologicals
- para-Aminobenzoates
- Peripheral Nervous System Agents
- Sensory Organs
- Sensory System Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Vasoprotectives
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzoic acid esters. These are ester derivatives of benzoic acid.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Benzoic acids and derivatives
- Direct Parent
- Benzoic acid esters
- Alternative Parents
- Aminobenzoic acids and derivatives / Benzoyl derivatives / Aniline and substituted anilines / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Primary amines / Organopnictogen compounds / Organooxygen compounds show 2 more
- Substituents
- Amine / Amino acid or derivatives / Aminobenzoic acid or derivatives / Aniline or substituted anilines / Aromatic homomonocyclic compound / Benzoate ester / Benzoyl / Carboxylic acid derivative / Carboxylic acid ester / Hydrocarbon derivative show 10 more
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- tertiary amino compound, substituted aniline, benzoate ester (CHEBI:8430)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 4Z8Y51M438
- CAS number
- 59-46-1
- InChI Key
- MFDFERRIHVXMIY-UHFFFAOYSA-N
- InChI
- InChI=1S/C13H20N2O2/c1-3-15(4-2)9-10-17-13(16)11-5-7-12(14)8-6-11/h5-8H,3-4,9-10,14H2,1-2H3
- IUPAC Name
- 2-(diethylamino)ethyl 4-aminobenzoate
- SMILES
- CCN(CC)CCOC(=O)C1=CC=C(N)C=C1
References
- Synthesis Reference
- US812554
- General References
- External Links
- Human Metabolome Database
- HMDB0014859
- KEGG Drug
- D08422
- KEGG Compound
- C07375
- PubChem Compound
- 4914
- PubChem Substance
- 46507724
- ChemSpider
- 4745
- BindingDB
- 64452
- 8701
- ChEBI
- 8430
- ChEMBL
- CHEMBL569
- ZINC
- ZINC000001530757
- Therapeutic Targets Database
- DAP000296
- PharmGKB
- PA451110
- Guide to Pharmacology
- GtP Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Procaine
- MSDS
- Download (73.1 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Prevention Hypotension 1 somestatus stop reason just information to hide 3 Completed Treatment Infection / Sepsis / Sepsis, Neonatal 1 somestatus stop reason just information to hide 3 Terminated Treatment Acute Otitis Media (AOM) / Pain 1 somestatus stop reason just information to hide 3 Unknown Status Treatment Bacterial Infections / Newborn, Infant / Sepsis 1 somestatus stop reason just information to hide 2 Unknown Status Treatment Human Immunodeficiency Virus (HIV) Infections 2 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Eli lilly and co
- Consolidated pharmaceutical group inc
- King pharmaceuticals inc
- Parke davis div warner lambert co
- Pfizer laboratories div pfizer inc
- Hospira inc
- Abraxis pharmaceutical products
- Bel mar laboratories inc
- Elkins sinn div ah robins co inc
- Gd searle llc
- Miles laboratories inc
- Watson laboratories inc
- Packagers
- APP Pharmaceuticals
- Hospira Inc.
- King Pharmaceuticals Inc.
- Merit Pharmaceuticals
- Monarch Pharmacy
- Physicians Total Care Inc.
- Prescript Pharmaceuticals
- Smiths Medical ASD Inc.
- Spectrum Pharmaceuticals
- Torrance Co.
- Dosage Forms
Form Route Strength Injection Other Injection Other 16 mmol/20ml Injection, solution, concentrate Intravenous Solution Dental Injection, solution Interstitial 1 % Injection, solution Interstitial 2 % Injection, solution Infiltration 10 mg/1mL Injection, solution Infiltration 20 mg/1mL Solution Infiltration 2 % Liquid Infiltration 2 % Injection, solution Intraspinal; Intrathecal; Subarachnoid 100 mg/1mL Injection, solution Intramuscular Injection, solution Intramuscular 100 mg/10ml Solution / drops Auricular (otic) Solution Intramuscular 20 mg Injection Parenteral 10 mg Solution Intramuscular 10 mg Solution Intramuscular 1 g Crystal Not applicable 1 g/1g Lotion Topical 2 % Solution Parenteral 20.00 mg Solution Infiltration 18 mg Solution Infiltration 36 mg Solution Parenteral 0.036 g Solution Infiltration 0.01 g Concentrate Intravenous drip Cream Topical Solution Intramuscular; Subcutaneous 10 mg Solution Parenteral 20 mg - Prices
Unit description Cost Unit Novocain 10% ampul 2.4USD ml Novocain 1% ampul 1.79USD ml Procaine hcl crystals 1.76USD g Nesacaine-mpf 3% vial 1.34USD ml Nesacaine-mpf 2% vial 1.28USD ml Nesacaine 2% vial 0.74USD ml Nesacaine 1% vial 0.72USD ml Chloroprocaine 3% vial 0.33USD ml Chloroprocaine 2% vial 0.26USD ml Procaine hcl 2% vial 0.15USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 61 °C PhysProp water solubility 9450 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 2.14 AVDEEF,A (1997) logS -1.4 ADME Research, USCD pKa 8.05 (at 15 °C) PERRIN,DD (1965) - Predicted Properties
Property Value Source Water Solubility 6.81 mg/mL ALOGPS logP 2.1 ALOGPS logP 1.88 Chemaxon logS -1.5 ALOGPS pKa (Strongest Basic) 8.96 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 55.56 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 70.3 m3·mol-1 Chemaxon Polarizability 26.81 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9747 Blood Brain Barrier + 0.9533 Caco-2 permeable + 0.6291 P-glycoprotein substrate Substrate 0.587 P-glycoprotein inhibitor I Non-inhibitor 0.9492 P-glycoprotein inhibitor II Non-inhibitor 0.9884 Renal organic cation transporter Non-inhibitor 0.684 CYP450 2C9 substrate Non-substrate 0.8646 CYP450 2D6 substrate Non-substrate 0.6643 CYP450 3A4 substrate Non-substrate 0.6456 CYP450 1A2 substrate Non-inhibitor 0.6308 CYP450 2C9 inhibitor Non-inhibitor 0.9312 CYP450 2D6 inhibitor Inhibitor 0.8932 CYP450 2C19 inhibitor Non-inhibitor 0.9294 CYP450 3A4 inhibitor Non-inhibitor 0.8308 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7918 Ames test Non AMES toxic 0.6165 Carcinogenicity Non-carcinogens 0.6462 Biodegradation Not ready biodegradable 0.9449 Rat acute toxicity 2.5160 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8728 hERG inhibition (predictor II) Non-inhibitor 0.6234
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 161.6701545 predictedDarkChem Lite v0.1.0 [M-H]- 155.83116 predictedDeepCCS 1.0 (2019) [M+H]+ 162.1149545 predictedDarkChem Lite v0.1.0 [M+H]+ 158.18916 predictedDeepCCS 1.0 (2019) [M+Na]+ 163.4690545 predictedDarkChem Lite v0.1.0 [M+Na]+ 164.35338 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms
- Specific Function
- transmembrane transporter binding
- Gene Name
- SCN10A
- Uniprot ID
- Q9Y5Y9
- Uniprot Name
- Sodium channel protein type 10 subunit alpha
- Molecular Weight
- 220623.605 Da
References
- Brau ME, Vogel W, Hempelmann G: Fundamental properties of local anesthetics: half-maximal blocking concentrations for tonic block of Na+ and K+ channels in peripheral nerve. Anesth Analg. 1998 Oct;87(4):885-9. [Article]
- Katalymov LL: [The effect of inhibitors of sodium permeability (novocaine and tetrodotoxin) on the trace depolarization of myelinated nerve fibers]. Fiziol Zh Im I M Sechenova. 1995 Sep;81(9):127-33. [Article]
- Creveling CR, Bell ME, Burke TR Jr, Chang E, Lewandowski-Lovenberg GA, Kim CH, Rice KC, Daly JW: Procaine isothiocyanate: an irreversible inhibitor of the specific binding of [3H]batrachotoxinin-A benzoate to sodium channels. Neurochem Res. 1990 Apr;15(4):441-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. During the development of neural circuits, plays a role in the synaptic refinement period, restricting spine maturation and growth. By competing with GIT1 interaction with ARHGEF7/beta-PIX, may reduce GIT1/ARHGEF7-regulated local activation of RAC1, hence affecting signaling and limiting the maturation and growth of inactive synapses. May also play a role in PPP2CB-NMDAR mediated signaling mechanism
- Specific Function
- calcium channel activity
- Gene Name
- GRIN3A
- Uniprot ID
- Q8TCU5
- Uniprot Name
- Glutamate receptor ionotropic, NMDA 3A
- Molecular Weight
- 125464.07 Da
References
- Hahnenkamp K, Durieux ME, Hahnenkamp A, Schauerte SK, Hoenemann CW, Vegh V, Theilmeier G, Hollmann MW: Local anaesthetics inhibit signalling of human NMDA receptors recombinantly expressed in Xenopus laevis oocytes: role of protein kinase C. Br J Anaesth. 2006 Jan;96(1):77-87. Epub 2005 Nov 18. [Article]
- Nishizawa N, Shirasaki T, Nakao S, Matsuda H, Shingu K: The inhibition of the N-methyl-D-aspartate receptor channel by local anesthetics in mouse CA1 pyramidal neurons. Anesth Analg. 2002 Feb;94(2):325-30, table of contents. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons
- Specific Function
- excitatory extracellular ligand-gated monoatomic ion channel activity
- Gene Name
- HTR3A
- Uniprot ID
- P46098
- Uniprot Name
- 5-hydroxytryptamine receptor 3A
- Molecular Weight
- 55279.835 Da
References
- Fan P, Weight FF: Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons. Neuropharmacology. 1994 Dec;33(12):1573-9. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Mediates sodium- and chloride-dependent transport of dopamine (PubMed:10375632, PubMed:11093780, PubMed:1406597, PubMed:15505207, PubMed:19478460, PubMed:8302271). Also mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (By similarity). Regulator of light-dependent retinal hyaloid vessel regression, downstream of OPN5 signaling (By similarity)
- Specific Function
- amine binding
- Gene Name
- SLC6A3
- Uniprot ID
- Q01959
- Uniprot Name
- Sodium-dependent dopamine transporter
- Molecular Weight
- 68494.255 Da
References
- Sato T, Kitayama S, Mitsuhata C, Ikeda T, Morita K, Dohi T: Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics. Naunyn Schmiedebergs Arch Pharmacol. 2000 Feb;361(2):214-20. [Article]
- Wilcox KM, Kimmel HL, Lindsey KP, Votaw JR, Goodman MM, Howell LL: In vivo comparison of the reinforcing and dopamine transporter effects of local anesthetics in rhesus monkeys. Synapse. 2005 Dec 15;58(4):220-8. [Article]
- Kiyatkin EA, Brown PL: The role of peripheral and central sodium channels in mediating brain temperature fluctuations induced by intravenous cocaine. Brain Res. 2006 Oct 30;1117(1):38-53. Epub 2006 Sep 7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane
- Specific Function
- acetylcholine receptor activity
- Gene Name
- CHRNA2
- Uniprot ID
- Q15822
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-2
- Molecular Weight
- 59764.82 Da
References
- Wang H, Zhang Y, Li ST: The effect of local anesthetics on the inhibition of adult muscle-type nicotinic acetylcholine receptors by nondepolarizing muscle relaxants. Eur J Pharmacol. 2010 Mar 25;630(1-3):29-33. doi: 10.1016/j.ejphar.2009.12.028. Epub 2010 Jan 4. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Blocker
- General Function
- Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+) (PubMed:14523450, PubMed:29330545, PubMed:31152168). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX)
- Specific Function
- actin binding
Components:
References
- Benham CD, Bolton TB, Lang RJ, Takewaki T: The mechanism of action of Ba2+ and TEA on single Ca2+-activated K+ -channels in arterial and intestinal smooth muscle cell membranes. Pflugers Arch. 1985 Feb;403(2):120-7. [Article]
- Ahn HY, Karaki H: Inhibitory effects of procaine on contraction and calcium movement in vascular and intestinal smooth muscles. Br J Pharmacol. 1988 Jul;94(3):789-96. doi: 10.1111/j.1476-5381.1988.tb11590.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Has primarily calcium-dependent phospholipase and lysophospholipase activities, with a major role in membrane lipid remodeling and biosynthesis of lipid mediators of the inflammatory response (PubMed:10358058, PubMed:14709560, PubMed:16617059, PubMed:17472963, PubMed:18451993, PubMed:27642067, PubMed:7794891, PubMed:8619991, PubMed:8702602, PubMed:9425121). Plays an important role in embryo implantation and parturition through its ability to trigger prostanoid production (By similarity). Preferentially hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids (phospholipase A2 activity) (PubMed:10358058, PubMed:17472963, PubMed:18451993, PubMed:7794891, PubMed:8619991, PubMed:9425121). Selectively hydrolyzes sn-2 arachidonoyl group from membrane phospholipids, providing the precursor for eicosanoid biosynthesis via the cyclooxygenase pathway (PubMed:10358058, PubMed:17472963, PubMed:18451993, PubMed:7794891, PubMed:9425121). In an alternative pathway of eicosanoid biosynthesis, hydrolyzes sn-2 fatty acyl chain of eicosanoid lysophopholipids to release free bioactive eicosanoids (PubMed:27642067). Hydrolyzes the ester bond of the fatty acyl group attached at sn-1 position of phospholipids (phospholipase A1 activity) only if an ether linkage rather than an ester linkage is present at the sn-2 position. This hydrolysis is not stereospecific (PubMed:7794891). Has calcium-independent phospholipase A2 and lysophospholipase activities in the presence of phosphoinositides (PubMed:12672805). Has O-acyltransferase activity. Catalyzes the transfer of fatty acyl chains from phospholipids to a primary hydroxyl group of glycerol (sn-1 or sn-3), potentially contributing to monoacylglycerol synthesis (PubMed:7794891)
- Specific Function
- calcium ion binding
- Gene Name
- PLA2G4A
- Uniprot ID
- P47712
- Uniprot Name
- Cytosolic phospholipase A2
- Molecular Weight
- 85238.2 Da
References
- Kunze H, Nahas N, Traynor JR, Wurl M: Effects of local anaesthetics on phospholipases. Biochim Biophys Acta. 1976 Jul 20;441(1):93-102. [Article]
- Hendrickson HS: The penetration of local anesthetics into phosphatidylcholine monolayers. J Lipid Res. 1976 Jul;17(4):393-8. [Article]
- Hendrickson HS, van Dam-Mieras MC: Local anesthetic inhibition of pancreatic phospholipase A2 action on lecithin monolayers. J Lipid Res. 1976 Jul;17(4):399-405. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Exhibits lysophospholipase, transacylase, PAF acetylhydrolase and asparaginase activities (By similarity). Can catalyze three types of transacylation reactions: (1) acyl transfer from 1-acyl-sn-glycero-3-phosphocholine (1-acyl-GPC) to the sn-1(3) positions of glycerol and 2-acylglycerol (sn-1 to -1(3) transfer), (2) acyl transfer from 1-acyl-GPC to the sn-2 positions of 1-acyl-GPC, 1-acyl-sn-glycero-3-phosphoethanolamine (1-acyl-GPE), and other lysophospholipids (sn-1 to -2 transfer) and (3) acyl transfer from 2-acyl-GPC to the sn-1 position of 2-acyl-GPC and 2-acyl-GPE (sn-2 to -1 transfer) (By similarity). Mediates the synthesis of 1-arachidonoyl species of phospholipids by transferring the arachidonoyl residue from 2-arachidonoyl lysophospholipid to the sn-1 position of 2-acyl lysophospholipid (By similarity)
- Specific Function
- 1-alkyl-2-acetylglycerophosphocholine esterase activity
- Gene Name
- ASPG
- Uniprot ID
- Q86U10
- Uniprot Name
- 60 kDa lysophospholipase
- Molecular Weight
- 60882.4 Da
References
- Kawashima Y, Nakagawa M, Suzuki Y, Uchiyama M: The relationship between chain elongation of palmitoyl-CoA and phospholipid content in rat liver microsomes. Biochim Biophys Acta. 1976 Aug 23;441(2):173-80. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:18391214, PubMed:20493079, PubMed:24169519, PubMed:8316221). Preferentially oxidizes serotonin (PubMed:20493079, PubMed:24169519). Also catalyzes the oxidative deamination of kynuramine to 3-(2-aminophenyl)-3-oxopropanal that can spontaneously condense to 4-hydroxyquinoline (By similarity)
- Specific Function
- aliphatic amine oxidase activity
Components:
References
- MacFarlane MD: Procaine HCl (Gerovital H3): a weak, reversible, fully competitive inhibitor of monoamine oxidase. Fed Proc. 1975 Jan;34(1):108-10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Methylates CpG residues. Preferentially methylates hemimethylated DNA. Associates with DNA replication sites in S phase maintaining the methylation pattern in the newly synthesized strand, that is essential for epigenetic inheritance. Associates with chromatin during G2 and M phases to maintain DNA methylation independently of replication. It is responsible for maintaining methylation patterns established in development. DNA methylation is coordinated with methylation of histones. Mediates transcriptional repression by direct binding to HDAC2. In association with DNMT3B and via the recruitment of CTCFL/BORIS, involved in activation of BAG1 gene expression by modulating dimethylation of promoter histone H3 at H3K4 and H3K9. Probably forms a corepressor complex required for activated KRAS-mediated promoter hypermethylation and transcriptional silencing of tumor suppressor genes (TSGs) or other tumor-related genes in colorectal cancer (CRC) cells (PubMed:24623306). Also required to maintain a transcriptionally repressive state of genes in undifferentiated embryonic stem cells (ESCs) (PubMed:24623306). Associates at promoter regions of tumor suppressor genes (TSGs) leading to their gene silencing (PubMed:24623306). Promotes tumor growth (PubMed:24623306)
- Specific Function
- DNA (cytosine-5-)-methyltransferase activity
- Gene Name
- DNMT1
- Uniprot ID
- P26358
- Uniprot Name
- DNA (cytosine-5)-methyltransferase 1
- Molecular Weight
- 183163.635 Da
References
- Villar-Garea A, Fraga MF, Espada J, Esteller M: Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells. Cancer Res. 2003 Aug 15;63(16):4984-9. [Article]
- Li YC, Wang Y, Li DD, Zhang Y, Zhao TC, Li CF: Procaine is a specific DNA methylation inhibitor with anti-tumor effect for human gastric cancer. J Cell Biochem. 2018 Feb;119(2):2440-2449. doi: 10.1002/jcb.26407. Epub 2017 Oct 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Required for genome-wide de novo methylation and is essential for the establishment of DNA methylation patterns during development (PubMed:12138111, PubMed:16357870, PubMed:30478443). DNA methylation is coordinated with methylation of histones (PubMed:12138111, PubMed:16357870, PubMed:30478443). It modifies DNA in a non-processive manner and also methylates non-CpG sites (PubMed:12138111, PubMed:16357870, PubMed:30478443). May preferentially methylate DNA linker between 2 nucleosomal cores and is inhibited by histone H1 (By similarity). Plays a role in paternal and maternal imprinting (By similarity). Required for methylation of most imprinted loci in germ cells (By similarity). Acts as a transcriptional corepressor for ZBTB18 (By similarity). Recruited to trimethylated 'Lys-36' of histone H3 (H3K36me3) sites (By similarity). Can actively repress transcription through the recruitment of HDAC activity (By similarity). Also has weak auto-methylation activity on Cys-710 in absence of DNA (By similarity)
- Specific Function
- chromatin binding
- Gene Name
- DNMT3A
- Uniprot ID
- Q9Y6K1
- Uniprot Name
- DNA (cytosine-5)-methyltransferase 3A
- Molecular Weight
- 101857.595 Da
References
- Li YC, Wang Y, Li DD, Zhang Y, Zhao TC, Li CF: Procaine is a specific DNA methylation inhibitor with anti-tumor effect for human gastric cancer. J Cell Biochem. 2018 Feb;119(2):2440-2449. doi: 10.1002/jcb.26407. Epub 2017 Oct 27. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters
- Specific Function
- acetylcholinesterase activity
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Perez-Guillermo F, Delgado EM, Vidal CJ: Inhibition of human serum and rabbit muscle cholinesterase by local anesthetics. Biochem Pharmacol. 1987 Nov 1;36(21):3593-6. [Article]
- Dorokhov KE, Grigorian GL: [Binding of reversible spin-labeled inhibitors with an butyrylcholinesterase active center]. Biofizika. 1986 Sep-Oct;31(5):746-51. [Article]
- Dhananjeyan MR, Trendel JA, Bykowski C, Sarver JG, Ando H, Erhardt PW: Rapid and sensitive HPLC assay for simultaneous determination of procaine and para-aminobenzoic acid from human and rat liver tissue extracts. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 May 15;867(2):247-52. doi: 10.1016/j.jchromb.2008.04.014. Epub 2008 Apr 29. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Mediates sodium- and chloride-dependent transport of dopamine (PubMed:10375632, PubMed:11093780, PubMed:1406597, PubMed:15505207, PubMed:19478460, PubMed:8302271). Also mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (By similarity). Regulator of light-dependent retinal hyaloid vessel regression, downstream of OPN5 signaling (By similarity)
- Specific Function
- amine binding
- Gene Name
- SLC6A3
- Uniprot ID
- Q01959
- Uniprot Name
- Sodium-dependent dopamine transporter
- Molecular Weight
- 68494.255 Da
References
- Sato T, Kitayama S, Mitsuhata C, Ikeda T, Morita K, Dohi T: Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics. Naunyn Schmiedebergs Arch Pharmacol. 2000 Feb;361(2):214-20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (PubMed:2008212, PubMed:8125921). Can also mediate sodium- and chloride-dependent transport of dopamine (PubMed:11093780, PubMed:8125921)
- Specific Function
- actin binding
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
References
- Sato T, Kitayama S, Mitsuhata C, Ikeda T, Morita K, Dohi T: Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics. Naunyn Schmiedebergs Arch Pharmacol. 2000 Feb;361(2):214-20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Serotonin transporter that cotransports serotonin with one Na(+) ion in exchange for one K(+) ion and possibly one proton in an overall electroneutral transport cycle. Transports serotonin across the plasma membrane from the extracellular compartment to the cytosol thus limiting serotonin intercellular signaling (PubMed:10407194, PubMed:12869649, PubMed:21730057, PubMed:27049939, PubMed:27756841, PubMed:34851672). Essential for serotonin homeostasis in the central nervous system. In the developing somatosensory cortex, acts in glutamatergic neurons to control serotonin uptake and its trophic functions accounting for proper spatial organization of cortical neurons and elaboration of sensory circuits. In the mature cortex, acts primarily in brainstem raphe neurons to mediate serotonin uptake from the synaptic cleft back into the pre-synaptic terminal thus terminating serotonin signaling at the synapse (By similarity). Modulates mucosal serotonin levels in the gastrointestinal tract through uptake and clearance of serotonin in enterocytes. Required for enteric neurogenesis and gastrointestinal reflexes (By similarity). Regulates blood serotonin levels by ensuring rapid high affinity uptake of serotonin from plasma to platelets, where it is further stored in dense granules via vesicular monoamine transporters and then released upon stimulation (PubMed:17506858, PubMed:18317590). Mechanistically, the transport cycle starts with an outward-open conformation having Na1(+) and Cl(-) sites occupied. The binding of a second extracellular Na2(+) ion and serotonin substrate leads to structural changes to outward-occluded to inward-occluded to inward-open, where the Na2(+) ion and serotonin are released into the cytosol. Binding of intracellular K(+) ion induces conformational transitions to inward-occluded to outward-open and completes the cycle by releasing K(+) possibly together with a proton bound to Asp-98 into the extracellular compartment. Na1(+) and Cl(-) ions remain bound throughout the transport cycle (PubMed:10407194, PubMed:12869649, PubMed:21730057, PubMed:27049939, PubMed:27756841, PubMed:34851672). Additionally, displays serotonin-induced channel-like conductance for monovalent cations, mainly Na(+) ions. The channel activity is uncoupled from the transport cycle and may contribute to the membrane resting potential or excitability (By similarity)
- Specific Function
- actin filament binding
- Gene Name
- SLC6A4
- Uniprot ID
- P31645
- Uniprot Name
- Sodium-dependent serotonin transporter
- Molecular Weight
- 70324.165 Da
References
- Sato T, Kitayama S, Mitsuhata C, Ikeda T, Morita K, Dohi T: Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics. Naunyn Schmiedebergs Arch Pharmacol. 2000 Feb;361(2):214-20. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 21, 2024 12:53