Drug – bio-affecting and body treating compositions – Immunoglobulin – antiserum – antibody – or antibody fragment,... – Reduced antigenicity – reduced ability to bind complement – or...
Patent
1982-09-27
1984-12-18
Phillips, Delbert R.
Drug, bio-affecting and body treating compositions
Immunoglobulin, antiserum, antibody, or antibody fragment,...
Reduced antigenicity, reduced ability to bind complement, or...
A61K 3700
Patent
active
044890613
ABSTRACT:
Peptides which are LRF analogs that inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads can be effective to suppress androgen-dependent behavior when administered to male mammals. The peptides are LRF antagonists having a binding affinity at least about 15 times that exhibited by LRF and having an ICR.sub.50 of less than 1/1. Examples of peptides which may be used are those having the structure:
R.sub.1 -R.sub.2 -R.sub.3 -D-Trp-Ser-Tyr-R.sub.4 -Leu-Arg-Pro-Gly-NH.sub.2 wherein R.sub.1 is selected from the group consisting of hydrogen, formyl, acetyl, acrylyl, benzoyl and allyl; R.sub.2 is selected from the group consisting of dehydro Pro, dehydro D-Pro, Thz and D-Thz; R.sub.3 is selected from the group consisting of pCl-D-Phe, pF-D-Phe, pNO.sub.2 -D-Phe and 3,4 Cl-D-Phe; R.sub.4 is selected from the group consisting of D-Trp and (imBzl) D-His; and Leu may be substituted by N.alpha.MeLeu.
Effective suppression of androgen-dependent behavior is achieved at a daily dosage level of not more than about 3 mg. per Kg. of body weight.
REFERENCES:
patent: 4377574 (1983-03-01), Rivier et al.
Bowers, et al., Biochem. & Biophys. Res. Commun. 72, (1976) 1003-1007.
C. Rivier, et al., Endocrinology 108, (1981) 1998-2001.
Chem. Abstr. 94, (1981) 25238n, 41612k, 41539s.
Chem. Abstr. 95, (1981) 91232c.
Chem. Abstr. 89, (1978) 157886d.
R. Lind, et al., Reversible Inhibition of Spermatogenesis 305, 663-667.
Science 210, (1980) 93,94.
Acta Endocrinologica 91, (1979) 601-608.
Rivier Catherine L.
Rivier Jean E. F.
Vale, Jr. Wylie W.
Phillips Delbert R.
The Salk Institute for Biological Studies
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