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1. (WO2001005401) MELANOCORTIN RECEPTOR-3 LIGANDS TO TREAT SEXUAL DYSFUNCTION

Pub. No.:    WO/2001/005401    International Application No.:    PCT/US2000/019408
Publication Date: Fri Jan 26 00:59:59 CET 2001 International Filing Date: Fri Jul 14 01:59:59 CEST 2000
IPC: A61K 31/4184
A61K 31/454
A61K 38/06
A61K 38/07
A61K 38/08
A61K 38/33
G01N 33/566
Applicants: TREGA BIOSCIENCES, INC.
DINES, Kevin, C.
GAHMAN, Timothy, C.
GIRTEN, Beverly, E.
HITCHIN, Douglas, L.
HOLME, Kevin, R.
LANG, Hengyuan
SLIVKA, Sandra, R.
WATSON-STRAUGHAN, Karen, J.
TUTTLE, Ronald, R.
PEI, Yazhong
Inventors: DINES, Kevin, C.
GAHMAN, Timothy, C.
GIRTEN, Beverly, E.
HITCHIN, Douglas, L.
HOLME, Kevin, R.
LANG, Hengyuan
SLIVKA, Sandra, R.
WATSON-STRAUGHAN, Karen, J.
TUTTLE, Ronald, R.
PEI, Yazhong
Title: MELANOCORTIN RECEPTOR-3 LIGANDS TO TREAT SEXUAL DYSFUNCTION
Abstract:
Methods for treating sexual dysfunction, such as erectile dysfunction or sexual arousal disorder, with a compound having the generic formula X1-X2-(D)Phe-Arg-(D)Trp-X3. A particularly useful compound is HP-228, which has the formula Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH2. The invention also provides methods for selecting melanocortin receptor-3 ligands by determining whether a compound modulates the activity of MC-3 as an agonist or antagonist. These methods can be used to screen compound libraries for ligands to treat MC-3-associated conditions. Such conditions include sexual dysfunction, including erectile dysfunction and sexual arousal disorder.