Growth hormone releasing peptides
View Patent ↗Disclosed are peptide and peptidomimetic compounds generally according to formula (I), and pharmaceutically acceptable salts thereof, that are useful as GHRP analogs: R 1 -A 2 -A 3 -A 4 -A 5 -R 2 (I) or a pharmaceutically acceptable salt thereof, wherein: A 1 is Aib, Apc or Inp; A 2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A 3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A 4 is 2Fua, Om, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A 5 is Apc, Dab, Dap, Lys, Orn, or deleted; R 1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and R 2 is OH or NH 2 ; and pharmaceutical compositions and methods of use thereof.
1. A synthesized compound wherein said compound is
H-Inp-D-Bal-D-Trp-Phe-Apc-NH 2 ,
or a pharmaceutically acceptable salt thereof.
2. A method of determining a compound's ability to bind to a growth hormone secretagogue (GHS) receptor, said method comprising the step of measuring the ability of a compound to affect binding of a compound according to claim 1 to said receptor, to a fragment of said receptor comprising a ghrelin binding site, to a polypeptide comprising said fragment of said receptor, or to a derivative of said polypeptide comprising said fragment of said receptor.