Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- DPI-221
- DrugBank Accession Number
- DB06121
- Background
DPI-221 is an investigational drug and a selective agonist for the δ-opioid receptor.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for DPI-221 (DB06121)
- Weight
- Average: 487.663
Monoisotopic: 487.299891019 - Chemical Formula
- C31H38FN3O
- Synonyms
- 4-((.ALPHA.S)-.ALPHA.-((2S,5R)-2,5-DIMETHYL-4-(3-FLUOROBENZYL)-1-PIPERAZINYL)BENZYL)-N,N-DIETHYLBENZAMIDE
- BENZAMIDE, N,N-DIETHYL-4-((S)-((2S,5R)-4-((3-FLUOROPHENYL)METHYL)-2,5-DIMETHYL-1-PIPERAZINYL)PHENYLMETHYL)-
- N,N-DIETHYL-4-((S)-((2S,5R)-4-((3-FLUOROPHENYL)METHYL)-2,5-DIMETHYL-1-PIPERAZINYL)PHENYLMETHYL)BENZAMIDE
Pharmacology
- Indication
Investigated for use/treatment in urinary incontinence.
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Not Available
- Mechanism of action
The opioid receptor system constitutes three receptor subtypes, {delta}, µ, and {kappa}, and all three receptors play a role in bladder control and micturition events. There is a growing volume of information supporting a role for the {delta} receptor in these processes. DPI-221 is an opioid {delta} receptor agonist.
Target Actions Organism UDelta-type opioid receptor Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- 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
- Not Available
- 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.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- X9LJN69TFK
- CAS number
- 519058-15-2
- InChI Key
- KEXJLZMJVOTFOY-QEGDFHJFSA-N
- InChI
- InChI=1S/C31H38FN3O/c1-5-33(6-2)31(36)28-17-15-27(16-18-28)30(26-12-8-7-9-13-26)35-21-23(3)34(20-24(35)4)22-25-11-10-14-29(32)19-25/h7-19,23-24,30H,5-6,20-22H2,1-4H3/t23-,24+,30+/m1/s1
- IUPAC Name
- SMILES
- [H][C@](N1C[C@@]([H])(C)N(CC2=CC(F)=CC=C2)C[C@]1([H])C)(C1=CC=CC=C1)C1=CC=C(C=C1)C(=O)N(CC)CC
References
- General References
- Holt JD, Watson MJ, Chang JP, O'Neill SJ, Wei K, Pendergast W, Gengo PJ, Chang KJ: DPI-221 [4-((alpha-s)-alpha-((2s,5r)-2,5-dimethyl-4-(3-fluorobenzyl)-1-piperazinyl)benzyl )-N,N-diethylbenzamide]: a novel nonpeptide delta receptor agonist producing increased micturition interval in normal rats. J Pharmacol Exp Ther. 2005 Nov;315(2):601-8. Epub 2005 Jul 14. [Article]
- External Links
- ChemSpider
- 8067312
- ZINC
- ZINC000023247677
- Wikipedia
- DPI-221
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- G-protein coupled receptor that functions as a receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine
- Specific Function
- G protein-coupled enkephalin receptor activity
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
Drug created at November 18, 2007 18:30 / Updated at August 01, 2024 14:13