Detail of "78542-68-4"

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Depression and excitation induced in mice by two geometric isomers of (+)13,14-didehydro-20-methylcarboprostacyclin, FCE 22177 and FCE 22176

Depression and excitation induced in mice by two geometric isomers of (+)13,14-didehydro-20-methylcarboprostacyclin, FCE 22177 and FCE 22176. Comparison with effects on blood pressure and platelet aggregation. Caparrotta, L.; Ceserani, R.; Mongelli, N.; Santi-Soncin, E.; Ragazzi, E.; Fassina, G. (Dep. Pharmacol., Univ. Padova, Padua 35131, Italy). Prostaglandins, 33(3), 351-62 (English) 1987. CODEN: PRGLBA. ISSN: 0090-6980. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Two geometric isomers of a stable deriv. of PGI2, FCE 22177 (I)(5E) [78542-68-4] and FCE 22176 (5Z) [93379-83-0], were injected i.v.In this article, certain chemicals are used. Some of their cas registry numbers are 78542-68-4 and 93379-83-0 in mice (5-400 mg/kg) to investigate the effects at the central nervous system (CNS) level (Irwin's test). The synthetic mixt. of the 2 isomers (5E:5Z = 7:3) was also tested. Isomers 5E and 5Z induced opposite effects: 5E (similar to PGI2) was depressive, 5Z induced stimulation. The mixt. showed a strong depressive symptomatol. The 2 isomers and their mixt. induced motor uncoordination and impaired the performance of mice in the rotarod test (200 mg/kg i.v.). Mice were depressed after 5E and mixt.; but 5Z induced excitation, in accordance with Irwin's test. 5E and 5Z showed analogous effects on mean blood pressure (hypotension) and heart rate (increase) in normotensive rats, but 5E was 7-fold more active than 5Z. The 2 isomers showed analogous inhibitory effect on guinea pig platelet aggregation in vitro, but 5E was 30-fold more active than 5Z. Thus, the 2 geometric isomers have similar effects on blood pressure, heart rate, and platelet aggregation, even if differing quant. In contrast, 5E and 5Z have opposite effects at the CNS level on motor function and behavior. The data suggest the presence of 2 different sites of action for PGI2 in CNS (Ca2+ and adenylate cyclase linked). The 2 geometric isomers, may be useful for examg. PGI2 receptor sites in different tissues. .