Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin.

A region between residues 38 and 42 of the human cholecystokinin-A (CCK-A) receptor was shown to be involved in the binding of CCK but not in that of JMV 179 and JMV 180, two peptides closely related to CCK (Kennedy, K., Escrieut, C., Dufresne, M.

Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors.

SR 27897 is a new non-peptide antagonist of CCKA receptors: 1-[[2-(4-(2-chlorophenyl)thiazol-2-yl)aminocarbonyl] indolyl] acetic acid. This compound is a potent ligand for CCKA binding sites (rat pancreatic membranes, Ki = 0.2 nM) and is highly selective (CCKB and gastrin/CCKA IC50 ratios of 800 and 5000 respectively).

Biochemical and pharmacological activities of SR 26831, a potent and selective elastase inhibitor.

SR 26831 ([[5-(2-chloro-benzyl-2-(terbutyloxycarbonyl)]-4,5,6,7- tetrahydrothieno(3,2-c)pyridine]N-oxide) is the first member of a new class of human leukocyte elastase inhibitors. SR 26831 inhibited in a dose-dependent manner elastases from human leukocytes or pancreas with IC50 values of 80 +/- 2.6 nM and 4.

Enhancement of neurite outgrowth from central nervous system neurons in primary culture by thrombin inhibitors.

Previous studies have shown that serine protease inhibitors promote neurite outgrowth from neuroblastoma cells, sympathetic neurons and sensory ganglia in culture. In the present study, a neurite promoting activity of thrombin inhibitors such as hirudin, D-Phe,Pro,Arg-CH2Cl, and paraamidinophenylalanine derivatives, was found in rat embryo (E17) septal neurons in primary culture. In contrast, no effect was shown on choline acetyltransferase activity of septal fragments in culture.