Linear free-sulfhydryl-containing oligopeptide derivatives as antihypertensive agents
US5106834A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 27, 1988 |
| Grant date | Apr 21, 1992 |
| Priority date | — |
| Expiry date | Dec 27, 2008 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Synthesis and use of novel oligopeptides are described, many of which peptides contain one or several unnatural amino acids. These short linear peptide derivatives are characterized by the presence of a free sulfhydryl function. These compounds have a high affinity for the Atrial Natriuretic Peptide (ANP) receptor coupled to particulate guanylate cyclase. Such peptides are full agonists at the ANP receptor as demonstrated by the ability of the peptides to stimulate the production of cGMP and to relax smooth muscles in vitro. In accord with these observations, the compounds of the invention lower blood pressure in mammals. Preferred peptides are the following: PA0 Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; and Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH.sub.2.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.