Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists

Autor:	Dhanoa Daljit S, Aleksandr K. Rabinovich, John M. May, David Robert Luthin, Dilip R. Bhumralkar, Richard A. Bychowski, Kenna L. Youngblood
Rok vydání:	1999
Předmět:	Male endocrine system Stereochemistry medicine.drug_class Clinical Biochemistry Carboxylic Acids Pharmaceutical Science Carboxamide Transfection Biochemistry Chemical synthesis Receptors Corticotropin-Releasing Hormone Corticotropin-releasing hormone receptor 1 Adrenocorticotropic Hormone In vivo Drug Discovery medicine Cyclic AMP Animals Humans Receptor Molecular Biology Cells Cultured Chemistry Organic Chemistry Antagonist Biological activity In vitro Rats Pituitary Gland Quinazolines Molecular Medicine hormones hormone substitutes and hormone antagonists
Zdroj:	Bioorganicmedicinal chemistry letters. 9(5)
ISSN:	0960-894X
Popis:	A novel series of derivatives of oxo-7H-benzo[e]perimidine-4-carboxylic acid (I) potently displaced radioligand binding of 125I-CRF to both CRF1 and CRF2 receptors. The members of this series antagonized CRF-stimulated cAMP formation and CRF-stimulated corticotropin release from rat pituitary in vivo. These are the first nonpeptide antagonists to show activity at both CRF1 and CRF2 receptors.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e6932047f37d506a62ba183cc103222 https://pubmed.ncbi.nlm.nih.gov/10201844 Zobrazit plný text záznamu Full Text from ScienceDirect