Detail of "5638-76-6"

Reference

Antivertigo agents

Antivertigo agents. I. Structure-activity relationships of 2-(2-aminoethyl)pyridines. Shiozawa, Akira; Ichikawa, Yuhichiro; Komuro, Chikara; Idzu, Genichi; Ishikawa, Michio; Kurashige, Shuji; Miyazaki, Hiroshi; Yamanaka, Hiroshi; Sakamoto, Takao (Res.In this study， 90125-75-0 and 90126-02-6 are also used. Lab., Nippon Kayaku Co., Tokyo 115, Japan). Chem. Pharm. Bull., 32(2), 553-63 (English) 1984. CODEN: CPBTAL. ISSN: 0009-2363. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 27, 28 A series of 2-(2-aminoethyl)pyridines (I; R1 = H, Me, Et; R2 = MeNH, NH2, NMe2, pyrrolidino, piperidino, piperazino, or substituted piperazino) derived by the modification of the amine moiety in betahistine, 2-(2-methylaminoethyl)pyridine, was synthesized and evaluated for antivertigo action in terms of inhibitory activity against spontaneous nystagmus in cats. The structure-activity relationships between the amine moieties and antivertigo activities were investigated. The effects of substituents on the Ph ring of the 4-phenylpiperazine moiety were investigated by means of quant. regression anal. using various physicochem. parameters. The following equation gave the best correlation. Log(1/ID30) = 0.417 p + 0.166 MR - 1.473. In this series of compds., 1-(2-methoxyphenyl)-4-[2-(2-pyridyl)ethyl]piperazine [3965-87-5], 1-(2-methoxyphenyl)-4-[2-[2-(6-methyl)pyridyl]ethyl]piperazine [90125-57-8] and 1-(2-methoxyphenyl)-4-[2-[2-(5-ethyl)pyridyl]ethyl]piperazine (II) [90125-58-9] showed more potent activity than betahistine [5638-76-6]. Thus, the 4-(2-methoxyphenyl)piperazine group was the most effective amine moiety for activity against spontaneous nystagmus. .

The characteristics of histamine H1-agonist-stimulated breakdown of inositol phospholipids differ between regions of guinea pig brain

The characteristics of histamine H1-agonist-stimulated breakdown of inositol phospholipids differ between regions of guinea pig brain. Carswell, Heather; Young, J. M. (Dep. Pharmacol., Univ. Cambridge, Cambridge CB2 2QD, UK). Biochem. Soc. Trans., 13(6), 1188-9 (English) 1985. CODEN: BCSTB5. ISSN: 0300-5127. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The 50% maximal effective concn. and the Hill coeff. from dose-response curves for histamine [51-45-6]-induced 3H-labeled inositol 1-phosphate [15421-51-9] accumulation from [3H]inositol-labeled lipids in guinea pig cerebral cortex slices were 20 mM and 1.1, resp.; whereas in cerebellar slices the corresponding values were 5 mM and 2.1. When expressed as a percentage of the max. response to histamine, the resp. responses to 2-methylhistamine [34392-54-6], Na,Na-dimethylhistamine [673-46-1], and betahistine [5638-76-6] were 32, 23, and 8% in cerebral cortex slices, 84, 72, and 52% in cerebellar slices, and 50, 37, and 19% in hippocampal slices. The regional variations in the response to histamine H1 agonists may due to the presence of a receptor reserve in the cerebellum and hippocampus or an indirect effect of H1 agonists in stimulating inositol phospholipid breakdown.