Pramlintide

Identification

Name
Pramlintide
Accession Number
DB01278
Description

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
Thumb
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.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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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.

TargetActionsOrganism
ACalcitonin receptor
agonist
Humans
AReceptor activity-modifying protein 1
agonist
Humans
AReceptor activity-modifying protein 2
agonist
Humans
AReceptor activity-modifying protein 3
agonist
Humans
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
Learn about our commercial Adverse Effects data.
Learn More
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
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.
DrugInteraction
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Pramlintide.
AcebutololThe therapeutic efficacy of Pramlintide can be increased when used in combination with Acebutolol.
AcetazolamideThe therapeutic efficacy of Pramlintide can be increased when used in combination with Acetazolamide.
AcetohexamideThe risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Pramlintide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Pramlintide can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Pramlintide.
AclidiniumThe risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Aclidinium.
AlbiglutideThe risk or severity of hypoglycemia can be increased when Pramlintide is combined with Albiglutide.
AlclometasoneThe risk or severity of hyperglycemia can be increased when Alclometasone is combined with Pramlintide.
AlogliptinThe risk or severity of hypoglycemia can be increased when Pramlintide is combined with Alogliptin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

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Food Interactions
  • Avoid alcohol. Ingesting alcohol may increase the risk of hypoglycemia.

Products

Product Ingredients
IngredientUNIICASInChI Key
Pramlintide acetate726I6TE06G196078-30-5NRKVKVQDUCJPIZ-MKAGXXMWSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
SymlinInjection0.6 mg/1mLSubcutaneousAmylin Pharmaceuticals, Inc.2006-10-102006-10-10US flag
SymlinInjection600 ug/1mLSubcutaneousPhysicians Total Care, Inc.2005-03-162011-12-31US flag
SymlinPenInjection1000 ug/1mLSubcutaneousAstraZeneca Pharmaceuticals LP2015-01-08Not applicableUS flag
SymlinPenInjection1000 ug/1mLSubcutaneousAstraZeneca Pharmaceuticals LP2015-01-08Not applicableUS flag
SymlinPenInjection1000 ug/1mLSubcutaneousAmylin Pharmaceuticals, Llc.2005-03-162017-07-31US flag
SymlinPenInjection1000 ug/1mLSubcutaneousAmylin Pharmaceuticals, Llc.2005-03-162016-08-31US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
A10BX05 — Pramlintide
Drug Categories
Classification
Not classified

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[[email protected]@H](CCCCN)C(=O)N[[email protected]]1CSSC[[email protected]](NC(=O)[[email protected]@]([H])(NC(=O)[[email protected]](C)NC(=O)[[email protected]@]([H])(NC(=O)[[email protected]](CC(N)=O)NC1=O)[[email protected]@H](C)O)[[email protected]@H](C)O)C(=O)N[[email protected]@H](C)C(=O)N[[email protected]@]([H])([[email protected]@H](C)O)C(=O)N[[email protected]@H](CCC(N)=O)C(=O)N[[email protected]@H](CCCNC(N)=N)C(=O)N[[email protected]@H](CC(C)C)C(=O)N[[email protected]@H](C)C(=O)N[[email protected]@H](CC(N)=O)C(=O)N[[email protected]@H](CC1=CC=CC=C1)C(=O)N[[email protected]@H](CC(C)C)C(=O)N[[email protected]@H](C(C)C)C(=O)N[[email protected]@H](CC1=CN=CN1)C(=O)N[[email protected]@H](CO)C(=O)N[[email protected]@H](CO)C(=O)N[[email protected]@H](CC(N)=O)C(=O)N[[email protected]@H](CC(N)=O)C(=O)N[[email protected]@H](CC1=CC=CC=C1)C(=O)NCC(=O)N1CCC[[email protected]]1C(=O)N[[email protected]@]([H])([[email protected]@H](C)CC)C(=O)N[[email protected]@H](CC(C)C)C(=O)N1CCC[[email protected]]1C(=O)N1CCC[[email protected]]1C(=O)N[[email protected]@]([H])([[email protected]@H](C)O)C(=O)N[[email protected]@H](CC(N)=O)C(=O)N[[email protected]@H](C(C)C)C(=O)NCC(=O)N[[email protected]@H](CO)C(=O)N[[email protected]@H](CC(N)=O)C(=O)N[[email protected]@]([H])([[email protected]@H](C)O)C(=O)N[[email protected]@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
  1. Jones MC: Therapies for diabetes: pramlintide and exenatide. Am Fam Physician. 2007 Jun 15;75(12):1831-5. [PubMed:17619527]
  2. 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. [PubMed:16330288]
  3. 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. [PubMed:18998755]
  4. Kleppinger EL, Vivian EM: Pramlintide for the treatment of diabetes mellitus. Ann Pharmacother. 2003 Jul-Aug;37(7-8):1082-9. [PubMed:12841822]
KEGG Drug
D05595
PubChem Substance
46509048
ChemSpider
44241191
RxNav
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
PhaseStatusPurposeConditionsCount
4CompletedOtherDiabetes / Schizoaffective Disorders / Schizophrenia / Weight Gain1
4CompletedTreatmentType 1 Diabetes Mellitus4
4CompletedTreatmentType 2 Diabetes Mellitus3
4Unknown StatusTreatmentEvidence of Previous Gastric Surgery / Hypoglycemia1
4WithdrawnTreatmentType 1 Diabetes Mellitus1
3CompletedTreatmentType 1 Diabetes Mellitus4
3CompletedTreatmentType 1 Diabetes Mellitus / Type 2 Diabetes Mellitus1
3Unknown StatusTreatmentType 1 Diabetes Mellitus1
3Unknown StatusTreatmentType 2 Diabetes Mellitus1
2CompletedTreatmentBMI >27 kg/m2 / BMI >30 kg/m24

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
FormRouteStrength
InjectionSubcutaneous0.6 mg/1mL
InjectionSubcutaneous600 ug/1mL
InjectionSubcutaneous1000 ug/1mL
Prices
Unit descriptionCostUnit
Symlin 600 mcg/ml Solution 5ml Vial227.69USD vial
SymlinPen 120 1000 mcg/ml Solution Two 2.7ml Syringes Per Box168.85USD syringe
Symlinpen 60 pen injector123.51USD ml
Symlin 0.6 mg/ml vial49.35USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6610824No2003-08-262011-03-03US flag
US5686411No1997-11-112019-03-16US flag
US5814600No1998-09-292015-09-29US flag
US6114304No2000-09-052017-09-05US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Liquid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
logP-28ChemAxon
pKa (Strongest Acidic)9.44ChemAxon
pKa (Strongest Basic)12.24ChemAxon
Physiological Charge4ChemAxon
Hydrogen Acceptor Count59ChemAxon
Hydrogen Donor Count56ChemAxon
Polar Surface Area1690.64 Å2ChemAxon
Rotatable Bond Count109ChemAxon
Refractivity983.93 m3·mol-1ChemAxon
Polarizability395.67 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Receptor activity
Specific 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 guanos...
Gene Name
CALCR
Uniprot ID
P30988
Uniprot Name
Calcitonin receptor
Molecular Weight
59351.865 Da
References
  1. 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. [PubMed:11772274]
  2. 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. [PubMed:19273748]
  3. 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. [PubMed:20357016]
  4. 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. [PubMed:20015292]
  5. 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. [PubMed:18593822]
  6. Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [PubMed:15494035]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Receptor activity
Specific 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.
Gene Name
RAMP1
Uniprot ID
O60894
Uniprot Name
Receptor activity-modifying protein 1
Molecular Weight
16987.765 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. 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. [PubMed:17016423]
  3. 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. [PubMed:11772274]
  4. 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. [PubMed:19273748]
  5. 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. [PubMed:20357016]
  6. 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. [PubMed:20015292]
  7. 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. [PubMed:18593822]
  8. Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [PubMed:15494035]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Protein transporter activity
Specific 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.
Gene Name
RAMP2
Uniprot ID
O60895
Uniprot Name
Receptor activity-modifying protein 2
Molecular Weight
19607.44 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. 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. [PubMed:17016423]
  3. 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. [PubMed:19273748]
  4. 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. [PubMed:20015292]
  5. 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. [PubMed:18593822]
  6. Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [PubMed:15494035]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Receptor activity
Specific 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 G...
Gene Name
RAMP3
Uniprot ID
O60896
Uniprot Name
Receptor activity-modifying protein 3
Molecular Weight
16518.325 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. 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. [PubMed:17016423]
  3. 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. [PubMed:11772274]
  4. 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. [PubMed:19273748]
  5. 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. [PubMed:20357016]
  6. 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. [PubMed:20015292]
  7. 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. [PubMed:18593822]
  8. Hay DL, Christopoulos G, Christopoulos A, Sexton PM: Amylin receptors: molecular composition and pharmacology. Biochem Soc Trans. 2004 Nov;32(Pt 5):865-7. [PubMed:15494035]

Drug created on May 16, 2007 16:15 / Updated on October 02, 2020 03:08

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