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Identification
- Summary
Pramlintide is an amylin analog used for the management of type 1 and type 2 diabetes mellitus as an adjunct to preprandial insulin therapy in patients without adequate glycemic control of insulin therapy.
- Brand Names
- Symlin
- Generic Name
- Pramlintide
- DrugBank Accession Number
- DB01278
- Background
Pramlintide is a relatively new adjunct treatment for diabetes (both type 1 and 2), developed by Amylin Pharmaceuticals. It is derived from amylin, a hormone that is released into the bloodstream, in a similar pattern as insulin, after a meal. Like insulin, amylin is deficient in individuals with diabetes.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Pramlintide (DB01278)
- Weight
- Average: 3949.44
Monoisotopic: 3946.920675009 - Chemical Formula
- C171H267N51O53S2
- Synonyms
- Pramlintide
- External IDs
- AC-0137
- AC-137
- AC0137
- AC137
Pharmacology
- Indication
For the treatment of type 1 and type 2 diabetes mellitus as an adjunct to preprandial insulin therapy in patients without adequate glycemic control of insulin therapy.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Type 1 diabetes •••••••••••• Management of Type 2 diabetes •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Pramlintide is a synthetic analog of amylin, a glucoregulatory hormone that is synthesized by pancreatic β-cells and released into the bloodstream, in a similar pattern as insulin, after a meal. Like insulin, amylin is deficient in individuals with diabetes. It is provided as an acetate salt. Pramlintide is a 37-amino acid polypeptide that differs structurally from human amylin by the replacement of alanine, serine, and serine at positions 25, 28, and 29 respectively with proline.
- Mechanism of action
Pramlintide is an amlyinomimetic, a functional analog of the naturally occurring pancreatic hormone amylin. Amylin has activity in a number of gastrointestinal and glucodynamic systems, and by mimicking its activity, pramlintide acts to improve glycemic control through modulation of the rate of gastric emptying, prevention of post-prandial rise in glucagon levels, and by increasing sensations of satiety, thereby reducing caloric intake and potentiating weight loss. There appears to be at least three distinct receptor complexes that bind with high affinity to amylin. All three complexes contain the calcitonin receptor at the core, plus one of three Receptor activity-modifying proteins, RAMP1, RAMP2, or RAMP3.
Target Actions Organism AGlucagon-like peptide 1 receptor agonistHumans ACalcitonin receptor agonistHumans AReceptor activity-modifying protein 1 agonistHumans AReceptor activity-modifying protein 2 agonistHumans AReceptor activity-modifying protein 3 agonistHumans - Absorption
The absolute bioavailability of a single subcutaneous dose of pramlintide is approximately 30 to 40%.
- Volume of distribution
Not Available
- Protein binding
Pramlintide does not extensively bind to blood cells or albumin (approximately 40% of the drug is unbound in plasma).
- Metabolism
Metabolized primarily by the kidneys.
- Route of elimination
Pramlintide is metabolized primarily by the kidneys.
- Half-life
Approximately 48 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
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Pramlintide. Acebutolol The therapeutic efficacy of Pramlintide can be increased when used in combination with Acebutolol. Acetazolamide The therapeutic efficacy of Pramlintide can be increased when used in combination with Acetazolamide. Acetohexamide The risk or severity of hypoglycemia can be increased when Pramlintide is combined with Acetohexamide. Acetyl sulfisoxazole The therapeutic efficacy of Pramlintide can be increased when used in combination with Acetyl sulfisoxazole. - Food Interactions
- Avoid alcohol. Ingesting alcohol may increase the risk of hypoglycemia.
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 Pramlintide acetate 726I6TE06G 196078-30-5 NRKVKVQDUCJPIZ-MKAGXXMWSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Symlin Injection 0.6 mg/1mL Subcutaneous Amylin Pharmaceuticals, Inc. 2006-10-10 2006-10-10 US 
Symlin Injection 600 ug/1mL Subcutaneous Physicians Total Care, Inc. 2005-03-16 2011-12-31 US SymlinPen Injection 1000 ug/1mL Subcutaneous AstraZeneca Pharmaceuticals LP 2015-01-08 2027-01-31 US SymlinPen Injection 1000 ug/1mL Subcutaneous Amylin Pharmaceuticals, Llc. 2005-03-16 2017-07-31 US SymlinPen Injection 1000 ug/1mL Subcutaneous AstraZeneca Pharmaceuticals LP 2015-01-08 2027-01-31 US
Categories
- ATC Codes
- A10BX05 — Pramlintide
- Drug Categories
- Alimentary Tract and Metabolism
- Amino Acids, Peptides, and Proteins
- Amylin Agonists
- Amylin Analog
- Amyloid
- Amyloidogenic Proteins
- Blood Glucose Lowering Agents
- Drugs Used in Diabetes
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypoglycemia-Associated Agents
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- Proteins
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- D3FM8FA78T
- CAS number
- 151126-32-8
- InChI Key
- TZIRZGBAFTZREM-MKAGXXMWSA-N
- InChI
- InChI=1S/C171H267N51O53S2/c1-21-81(12)130(163(268)207-110(56-78(6)7)169(274)222-53-33-42-118(222)170(275)221-52-32-41-117(221)160(265)219-135(89(20)230)167(272)206-109(66-125(180)238)151(256)212-128(79(8)9)161(266)186-68-126(239)192-111(70-223)154(259)203-107(64-123(178)236)152(257)218-134(88(19)229)166(271)195-98(136(181)241)57-92-43-45-94(231)46-44-92)214-159(264)116-40-31-51-220(116)127(240)69-187-141(246)101(58-90-34-24-22-25-35-90)199-148(253)105(62-121(176)234)201-149(254)106(63-122(177)235)202-155(260)112(71-224)209-156(261)113(72-225)208-146(251)103(60-93-67-184-75-188-93)205-162(267)129(80(10)11)213-150(255)100(55-77(4)5)198-145(250)102(59-91-36-26-23-27-37-91)200-147(252)104(61-120(175)233)196-137(242)82(13)189-144(249)99(54-76(2)3)197-142(247)96(39-30-50-185-171(182)183)193-143(248)97(47-48-119(174)232)194-165(270)132(86(17)227)215-138(243)83(14)190-157(262)114-73-276-277-74-115(210-140(245)95(173)38-28-29-49-172)158(263)204-108(65-124(179)237)153(258)217-131(85(16)226)164(269)191-84(15)139(244)216-133(87(18)228)168(273)211-114/h22-27,34-37,43-46,67,75-89,95-118,128-135,223-231H,21,28-33,38-42,47-66,68-74,172-173H2,1-20H3,(H2,174,232)(H2,175,233)(H2,176,234)(H2,177,235)(H2,178,236)(H2,179,237)(H2,180,238)(H2,181,241)(H,184,188)(H,186,266)(H,187,246)(H,189,249)(H,190,262)(H,191,269)(H,192,239)(H,193,248)(H,194,270)(H,195,271)(H,196,242)(H,197,247)(H,198,250)(H,199,253)(H,200,252)(H,201,254)(H,202,260)(H,203,259)(H,204,263)(H,205,267)(H,206,272)(H,207,268)(H,208,251)(H,209,261)(H,210,245)(H,211,273)(H,212,256)(H,213,255)(H,214,264)(H,215,243)(H,216,244)(H,217,258)(H,218,257)(H,219,265)(H4,182,183,185)/t81-,82-,83-,84-,85+,86+,87+,88+,89+,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,128-,129-,130-,131-,132-,133-,134-,135-/m0/s1
- IUPAC Name
- (2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-{[(1S)-1-{[(1S)-2-carbamoyl-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-2-carbamoyl-1-{[(1S)-2-carbamoyl-1-{[(1S)-1-({2-[(2S)-2-{[(1S,2S)-1-{[(2S)-1-[(2S)-2-[(2S)-2-{[(1S,2R)-1-{[(1S)-2-carbamoyl-1-{[(1S)-1-[({[(1S)-1-{[(1S)-2-carbamoyl-1-{[(1S,2R)-1-{[(1S)-1-carbamoyl-2-(4-hydroxyphenyl)ethyl]carbamoyl}-2-hydroxypropyl]carbamoyl}ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}methyl)carbamoyl]-2-methylpropyl]carbamoyl}ethyl]carbamoyl}-2-hydroxypropyl]carbamoyl}pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]carbamoyl}-2-methylbutyl]carbamoyl}pyrrolidin-1-yl]-2-oxoethyl}carbamoyl)-2-phenylethyl]carbamoyl}ethyl]carbamoyl}ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-(1H-imidazol-5-yl)ethyl]carbamoyl}-2-methylpropyl]carbamoyl}-3-methylbutyl]carbamoyl}-2-phenylethyl]carbamoyl}ethyl]carbamoyl}ethyl]carbamoyl}-3-methylbutyl]carbamoyl}butyl]-2-[(2S,3R)-2-[(2S)-2-{[(4R,7S,10S,13S,16S,19R)-16-(carbamoylmethyl)-19-[(2S)-2,6-diaminohexanamido]-7,13-bis[(1R)-1-hydroxyethyl]-10-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl]formamido}propanamido]-3-hydroxybutanamido]pentanediamide
- SMILES
- [H]N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@]([H])(NC(=O)[C@H](C)NC(=O)[C@@]([H])(NC(=O)[C@H](CC(N)=O)NC1=O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@]([H])([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@]([H])([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@]([H])([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@]([H])([C@@H](C)O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=O
References
- Synthesis Reference
Andreas Brunner, Oleg Werbitzky, Stephane Varray, Francesca Quattrini, Holger Hermann, Andrew Strong, Fernando Albericio, Judit Tulla-Puche, Yesica Garcia Ramos, "PROCESS FOR THE PRODUCTION OF PRAMLINTIDE." U.S. Patent US20100249370, issued September 30, 2010.
US20100249370- General References
- Jones MC: Therapies for diabetes: pramlintide and exenatide. Am Fam Physician. 2007 Jun 15;75(12):1831-5. [Article]
- Ryan GJ, Jobe LJ, Martin R: Pramlintide in the treatment of type 1 and type 2 diabetes mellitus. Clin Ther. 2005 Oct;27(10):1500-12. [Article]
- Edelman S, Maier H, Wilhelm K: Pramlintide in the treatment of diabetes mellitus. BioDrugs. 2008;22(6):375-86. doi: 10.2165/0063030-200822060-00004. [Article]
- Kleppinger EL, Vivian EM: Pramlintide for the treatment of diabetes mellitus. Ann Pharmacother. 2003 Jul-Aug;37(7-8):1082-9. [Article]
- External Links
- KEGG Drug
- D05595
- PubChem Substance
- 46509048
- ChemSpider
- 44241191
- 139953
- ChEBI
- 135922
- ChEMBL
- CHEMBL2103758
- Therapeutic Targets Database
- DCL000936
- PharmGKB
- PA164781394
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Pramlintide
- FDA label
- Download (856 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 data4 Completed Other Diabetes / Schizoaffective Disorders / Schizophrenia / Weight Gain 1 somestatus stop reason just information to hide 4 Completed Treatment Diabetes Mellitus, Insulin Dependent 1 somestatus stop reason just information to hide 4 Completed Treatment Evidence of Previous Gastric Surgery / Hypoglycemia 1 somestatus stop reason just information to hide 4 Completed Treatment Type 1 Diabetes Mellitus 3 somestatus stop reason just information to hide 4 Completed Treatment Type 2 Diabetes Mellitus 3 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Amylin Pharmaceuticals
- Baxter International Inc.
- CP Pharmaceuticals Ltd.
- Hollister-Stier Laboratories LLC
- OMJ Pharmaceuticals
- Physicians Total Care Inc.
- Quality Care
- Dosage Forms
Form Route Strength Injection Subcutaneous 0.6 mg/1mL Injection Subcutaneous 600 ug/1mL Injection Subcutaneous 1000 ug/1mL - Prices
Unit description Cost Unit Symlin 600 mcg/ml Solution 5ml Vial 227.69USD vial SymlinPen 120 1000 mcg/ml Solution Two 2.7ml Syringes Per Box 168.85USD syringe Symlinpen 60 pen injector 123.51USD ml Symlin 0.6 mg/ml vial 49.35USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6610824 No 2003-08-26 2011-03-03 US US5686411 No 1997-11-11 2019-03-16 US US5814600 No 1998-09-29 2015-09-29 US US6114304 No 2000-09-05 2017-09-05 US
Properties
- State
- Liquid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source logP -28 Chemaxon pKa (Strongest Acidic) 9.44 Chemaxon pKa (Strongest Basic) 12.24 Chemaxon Physiological Charge 4 Chemaxon Hydrogen Acceptor Count 59 Chemaxon Hydrogen Donor Count 56 Chemaxon Polar Surface Area 1690.64 Å2 Chemaxon Rotatable Bond Count 109 Chemaxon Refractivity 983.93 m3·mol-1 Chemaxon Polarizability 395.67 Å3 Chemaxon Number of Rings 8 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - 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
- Yes
- Actions
- Agonist
- General Function
- G-protein coupled receptor for glucagon-like peptide 1 (GLP-1) (PubMed:19861722, PubMed:26308095, PubMed:27196125, PubMed:28514449, PubMed:7517895, PubMed:8216285, PubMed:8405712). Ligand binding triggers activation of a signaling cascade that leads to the activation of adenylyl cyclase and increased intracellular cAMP levels (PubMed:19861722, PubMed:26308095, PubMed:27196125, PubMed:28514449, PubMed:7517895, PubMed:8216285, PubMed:8405712). Plays a role in regulating insulin secretion in response to GLP-1 (By similarity)
- Specific Function
- Glucagon receptor activity
- Gene Name
- GLP1R
- Uniprot ID
- P43220
- Uniprot Name
- Glucagon-like peptide 1 receptor
- Molecular Weight
- 53025.22 Da
References
- 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
- Agonist
- General Function
- This is a receptor for calcitonin. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. The calcitonin receptor is thought to couple to the heterotrimeric guanosine triphosphate-binding protein that is sensitive to cholera toxin
- Specific Function
- Amylin receptor activity
- Gene Name
- CALCR
- Uniprot ID
- P30988
- Uniprot Name
- Calcitonin receptor
- Molecular Weight
- 55344.175 Da
References
- Nyholm B, Brock B, Orskov L, Schmitz O: Amylin receptor agonists: a novel pharmacological approach in the management of insulin-treated diabetes mellitus. Expert Opin Investig Drugs. 2001 Sep;10(9):1641-52. [Article]
- Roth JD, Maier H, Chen S, Roland BL: Implications of amylin receptor agonism: integrated neurohormonal mechanisms and therapeutic applications. Arch Neurol. 2009 Mar;66(3):306-10. doi: 10.1001/archneurol.2008.581. [Article]
- Lutz TA: The role of amylin in the control of energy homeostasis. Am J Physiol Regul Integr Comp Physiol. 2010 Jun;298(6):R1475-84. doi: 10.1152/ajpregu.00703.2009. Epub 2010 Mar 31. [Article]
- Qi T, Hay DL: Structure-function relationships of the N-terminus of receptor activity-modifying proteins. Br J Pharmacol. 2010 Mar;159(5):1059-68. doi: 10.1111/j.1476-5381.2009.00541.x. Epub 2009 Dec 10. [Article]
- Qi T, Christopoulos G, Bailey RJ, Christopoulos A, Sexton PM, Hay DL: Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function. Mol Pharmacol. 2008 Oct;74(4):1059-71. doi: 10.1124/mol.108.047142. Epub 2008 Jul 1. [Article]
- Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) to the plasma membrane. Acts as a receptor for calcitonin-gene-related peptide (CGRP) together with CALCRL
- Specific Function
- Amylin receptor activity
- Gene Name
- RAMP1
- Uniprot ID
- O60894
- Uniprot Name
- Receptor activity-modifying protein 1
- Molecular Weight
- 16987.765 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Nyholm B, Brock B, Orskov L, Schmitz O: Amylin receptor agonists: a novel pharmacological approach in the management of insulin-treated diabetes mellitus. Expert Opin Investig Drugs. 2001 Sep;10(9):1641-52. [Article]
- Roth JD, Maier H, Chen S, Roland BL: Implications of amylin receptor agonism: integrated neurohormonal mechanisms and therapeutic applications. Arch Neurol. 2009 Mar;66(3):306-10. doi: 10.1001/archneurol.2008.581. [Article]
- Lutz TA: The role of amylin in the control of energy homeostasis. Am J Physiol Regul Integr Comp Physiol. 2010 Jun;298(6):R1475-84. doi: 10.1152/ajpregu.00703.2009. Epub 2010 Mar 31. [Article]
- Qi T, Hay DL: Structure-function relationships of the N-terminus of receptor activity-modifying proteins. Br J Pharmacol. 2010 Mar;159(5):1059-68. doi: 10.1111/j.1476-5381.2009.00541.x. Epub 2009 Dec 10. [Article]
- Qi T, Christopoulos G, Bailey RJ, Christopoulos A, Sexton PM, Hay DL: Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function. Mol Pharmacol. 2008 Oct;74(4):1059-71. doi: 10.1124/mol.108.047142. Epub 2008 Jul 1. [Article]
- Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) to the plasma membrane. Acts as a receptor for adrenomedullin (AM) together with CALCRL
- Specific Function
- Adrenomedullin binding
- Gene Name
- RAMP2
- Uniprot ID
- O60895
- Uniprot Name
- Receptor activity-modifying protein 2
- Molecular Weight
- 19607.44 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Roth JD, Maier H, Chen S, Roland BL: Implications of amylin receptor agonism: integrated neurohormonal mechanisms and therapeutic applications. Arch Neurol. 2009 Mar;66(3):306-10. doi: 10.1001/archneurol.2008.581. [Article]
- Qi T, Hay DL: Structure-function relationships of the N-terminus of receptor activity-modifying proteins. Br J Pharmacol. 2010 Mar;159(5):1059-68. doi: 10.1111/j.1476-5381.2009.00541.x. Epub 2009 Dec 10. [Article]
- Qi T, Christopoulos G, Bailey RJ, Christopoulos A, Sexton PM, Hay DL: Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function. Mol Pharmacol. 2008 Oct;74(4):1059-71. doi: 10.1124/mol.108.047142. Epub 2008 Jul 1. [Article]
- Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Plays a role in cardioprotection by reducing cardiac hypertrophy and perivascular fibrosis in a GPER1-dependent manner. Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) and GPER1 to the plasma membrane. Acts as a receptor for adrenomedullin (AM) together with CALCRL
- Specific Function
- Adrenomedullin receptor activity
- Gene Name
- RAMP3
- Uniprot ID
- O60896
- Uniprot Name
- Receptor activity-modifying protein 3
- Molecular Weight
- 16518.325 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Nyholm B, Brock B, Orskov L, Schmitz O: Amylin receptor agonists: a novel pharmacological approach in the management of insulin-treated diabetes mellitus. Expert Opin Investig Drugs. 2001 Sep;10(9):1641-52. [Article]
- Roth JD, Maier H, Chen S, Roland BL: Implications of amylin receptor agonism: integrated neurohormonal mechanisms and therapeutic applications. Arch Neurol. 2009 Mar;66(3):306-10. doi: 10.1001/archneurol.2008.581. [Article]
- Lutz TA: The role of amylin in the control of energy homeostasis. Am J Physiol Regul Integr Comp Physiol. 2010 Jun;298(6):R1475-84. doi: 10.1152/ajpregu.00703.2009. Epub 2010 Mar 31. [Article]
- Qi T, Hay DL: Structure-function relationships of the N-terminus of receptor activity-modifying proteins. Br J Pharmacol. 2010 Mar;159(5):1059-68. doi: 10.1111/j.1476-5381.2009.00541.x. Epub 2009 Dec 10. [Article]
- Qi T, Christopoulos G, Bailey RJ, Christopoulos A, Sexton PM, Hay DL: Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function. Mol Pharmacol. 2008 Oct;74(4):1059-71. doi: 10.1124/mol.108.047142. Epub 2008 Jul 1. [Article]
- Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [Article]
Drug created at May 16, 2007 22:15 / Updated at August 26, 2024 19:23