Identification

Name
Pramlintide
Accession Number
DB01278
Type
Small Molecule
Groups
Approved, Investigational
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.

Structure
Thumb
Synonyms
Not Available
External IDs
AC-0137 / AC-137 / AC0137 / AC137
Product Ingredients
IngredientUNIICASInChI Key
Pramlintide acetate726I6TE06G196078-30-5NRKVKVQDUCJPIZ-MKAGXXMWSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SymlinInjection600 ug/1mLSubcutaneousPhysicians Total Care, Inc.2005-03-162011-12-31Us
SymlinInjection0.6 mg/1mLSubcutaneousAmylin Pharmaceuticals, Inc.2006-10-102006-10-10Us
SymlinPenInjection1000 ug/1mLSubcutaneousAstra Zeneca Lp2015-01-08Not applicableUs
SymlinPenInjection1000 ug/1mLSubcutaneousAmylin Pharmaceuticals, Llc.2005-03-162017-07-31Us
SymlinPenInjection1000 ug/1mLSubcutaneousAstra Zeneca Lp2015-01-08Not applicableUs
SymlinPenInjection1000 ug/1mLSubcutaneousAmylin Pharmaceuticals, Llc.2005-03-162016-08-31Us
Categories
UNII
D3FM8FA78T
CAS number
151126-32-8
Weight
Average: 3949.44
Monoisotopic: 3946.920675009
Chemical Formula
C171H267N51O53S2
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

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
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
Human
AReceptor activity-modifying protein 1
agonist
Human
AReceptor activity-modifying protein 2
agonist
Human
AReceptor activity-modifying protein 3
agonist
Human
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
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Pramlintide is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Pramlintide can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Pramlintide.
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 acidAcetylsalicylic acid may increase the hypoglycemic activities of Pramlintide.
AclidiniumThe risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Aclidinium.
AgmatineThe risk or severity of hypoglycemia can be increased when Agmatine is combined with Pramlintide.
AICA ribonucleotideThe risk or severity of hypoglycemia can be increased when Pramlintide is combined with AICA ribonucleotide.
Food Interactions
Not Available

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]
External Links
KEGG Drug
D05595
PubChem Substance
46509048
ChemSpider
44241191
ChEBI
135922
ChEMBL
CHEMBL2103758
Therapeutic Targets Database
DCL000936
PharmGKB
PA164781394
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pramlintide
ATC Codes
A10BX05 — Pramlintide
FDA label
Download (856 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Enrolling by InvitationDiagnosticAlzheimer's Disease (AD) / Mild Cognitive Impairment (MCI)1
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
1RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
1, 2WithdrawnTreatmentDiabetes Mellitus (DM)1
2CompletedTreatmentBMI >27 kg/m2 / BMI >30 kg/m24
2CompletedTreatmentBMI >30 kg/m23
2CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent1
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Type 2 Diabetes Mellitus2
2TerminatedTreatmentBMI >30 kg/m21
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 14
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Type 2 Diabetes Mellitus1
3Unknown StatusTreatmentDiabetes, Diabetes Mellitus Type 11
3Unknown StatusTreatmentType 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentEvidence of Previous Gastric Surgery / Hypoglycemia1
4CompletedNot AvailableDiabetes Mellitus (DM) / Schizoaffective Disorders / Schizophrenic Disorders / Weight gain therapy1
4CompletedTreatmentDiabetes, Diabetes Mellitus Type 13
4CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus2
4Unknown StatusTreatmentType 2 Diabetes Mellitus1
4WithdrawnTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedNot AvailableDiabetes, Diabetes Mellitus Type 1 / Type 2 Diabetes Mellitus1
Not AvailableCompletedDiagnosticDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedHealth Services ResearchDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableUnknown StatusBasic ScienceBMI >30 kg/m21
Not AvailableWithdrawnTreatmentType 2 Diabetes Mellitus1

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)
US6610824No1994-03-032011-03-03Us
US5686411No1999-03-162019-03-16Us
US5814600No1995-09-292015-09-29Us
US6114304No1997-09-052017-09-05Us

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

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
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
Human
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
Human
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
Human
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 November 02, 2018 08:31