Abstract
We previously reported a series of benzazepine derivatives as orally active nonpeptide arginine vasopressin (AVP) V2 receptor antagonists. After the lead structure OPC-31260 was structurally evaluated and optimized, the introduction of the 7-Cl moiety on the benzazepine and 2-CH3 on the aminobenzoyl moiety enhanced its oral activity. The new AVP-V2 selective antagonist OPC-41061 was determined to be a potent and orally active agent.
MeSH terms
-
Animals
-
Antidiuretic Hormone Receptor Antagonists*
-
Arginine Vasopressin / metabolism
-
Benzazepines / chemistry
-
Benzazepines / metabolism
-
Benzazepines / pharmacology*
-
Diuretics / pharmacology
-
Magnetic Resonance Spectroscopy
-
Male
-
Molecular Structure
-
Radioligand Assay
-
Rats
-
Rats, Sprague-Dawley
-
Receptors, Vasopressin / metabolism
-
Tolvaptan
Substances
-
Antidiuretic Hormone Receptor Antagonists
-
Benzazepines
-
Diuretics
-
Receptors, Vasopressin
-
Arginine Vasopressin
-
Tolvaptan