Target Information

Target General Infomation
Target ID
T45457
Former ID
TTDR00057
Target Name
Melanocortin receptor
Target Type
Clinical Trial
Disease Erectile dysfunction [ICD9: 302.72, 607.84; ICD10: F52.2, N48.4]
Sexual dysfunction [ICD9: 302.7; ICD10: F52]
Ulcerative colitis [ICD9: 556; ICD10: K51]
Target Validation
T45457
Drugs and Mode of Action
Drug(s) Bremelanotide Drug Info Phase 3 Erectile dysfunction [536493]
Bremelanotide Drug Info Phase 2a Sexual dysfunction [536493]
ASP-3291 Drug Info Phase 2 Ulcerative colitis [523934]
Inhibitor Ac-His-DNal(2)-Arg-Trp-NH2 Drug Info [529699]
Ac-His-DPhe(3,4-diCl)-Arg-Trp-NH2 Drug Info [529699]
Ac-His-DPhe(pBr)-Arg-Trp-NH2 Drug Info [529699]
Ac-His-DPhe(pCF3)-Arg-Trp-NH2 Drug Info [529699]
Ac-His-DPhe(pI)-Arg-Trp-NH2 Drug Info [529699]
Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 Drug Info [530169]
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 Drug Info [530169]
Ac-YRC(Me)*EHdFRWC(Me)NH2 Drug Info [527529]
Ac-YRMEHdFRWG-NH2 Drug Info [527529]
Ac-YRMEHdFRWGSPPKD-NH2 Drug Info [527529]
Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 Drug Info [527529]
Ac-YR[CEH(pCl-dF)RWC]-NH2 Drug Info [527529]
Ac-YR[CEH(pF-dF)RWC]-NH2 Drug Info [527529]
AEKKDEGPYRMEHFRWGSPPKD Drug Info [527529]
Bremelanotide Drug Info [1725886]
C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-(CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
GPYRMEHFRWGSPPKD-NH2 Drug Info [527529]
MK-10 Drug Info [526348]
MK-11 Drug Info [526348]
NDP-SYSMEHFRWGKPVG Drug Info [527529]
Modulator ASP-3291 Drug Info [550606]
References
Ref 523934ClinicalTrials.gov (NCT01612039) Safety, Efficacy, and Tolerability Study of ASP3291 in Patients With Active Ulcerative Colitis. U.S. National Institutes of Health.
Ref 536493Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27.
Ref 526348J Med Chem. 2002 Jun 6;45(12):2644-50.Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 528082J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
Ref 529226J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
Ref 529699J Med Chem. 2008 Sep 25;51(18):5585-93.Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.
Ref 530169J Med Chem. 2009 Jun 25;52(12):3627-35.Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
Ref 550606Clinical pipeline report, company report or official report of Drais Pharmaceuticals.
Ref 1725886Wikipedia: Bremelanotide

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