7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1 H -1-benzazepine (OPC-41061): A potent, orally active nonpeptide arginine vasopressin V 2 receptor antagonist

Autor:	Hidenori Ogawa, Hiroshi Yamashita, Toyoki Mori, Hisashi Miyamoto, Michiaki Tominaga, Yoshitaka Yamamura, Kazumi Kondo, Kenji Nakaya, Toshiyuki Onogawa, Shigeki Nakamura, Kazuyoshi Kitano, Michinori Tanaka
Rok vydání:	1999
Předmět:	Male Receptors Vasopressin Vasopressin Magnetic Resonance Spectroscopy Arginine medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Benzazepine Rats Sprague-Dawley Radioligand Assay chemistry.chemical_compound Oral administration Arginine vasopressin receptor 2 Drug Discovery medicine Animals Moiety Diuretics Molecular Biology Molecular Structure Organic Chemistry Antagonist Benzazepines Rats Arginine Vasopressin stomatognathic diseases nervous system chemistry Tolvaptan Molecular Medicine Antidiuretic Hormone Receptor Antagonists hormones hormone substitutes and hormone antagonists
Zdroj:	Bioorganic & Medicinal Chemistry. 7:1743-1754
ISSN:	0968-0896
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c105b64436f8c1b59fe63905bd351123 https://doi.org/10.1016/s0968-0896(99)00101-7 Zobrazit plný text záznamu Full Text from ScienceDirect