Patent number: 4684620
Abstract: Novel compounds which are capable of binding with enhanced specificity to the mu opioid receptor are disclosed. The compounds are analogs of somatostain and have the formula: ##STR1## wherein X is CONH.sub.2 or CH.sub.2 OH;Y and Z are independently sulfur or CH.sub.2 ;R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, methyl, ethyl, cyclopentamethylene, or a lower alkyl group having five or less carbon atoms;R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, methyl, ethyl, cyclopentamethylene, or a lower alkyl group having five or less carbon atoms, provided, however, that R.sup.1, R.sup.2, R.sup.3, and R.sup.4 may not all be hydrogen;AA.sub.1 is Phe, D-Phe, phenyl-Gly, D-phenyl-Gly, Tyr, D-Tyr, L-1-Naphthylalanine, D-1-Naphthylalanine, or D-Phe(4-Me);AA.sub.2 is Tyr, Phe, Tyr(OMe), Phe(4-Me),Tyr(OEt), or Phe(4-Et); andAA.sub.3 is Lys, Arg, Orn or homo-Arg.
Type:
Grant
Filed:
September 4, 1984
Date of Patent:
August 4, 1987
Assignee:
Gibson-Stephens Neuropharmaceuticals, Inc.
Inventors:
Victor J. Hruby, John T. Pelton