Detail of "57536-86-4"

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Evidence that blood pressure reduction by serotonin antagonists is related to alpha receptor blockade in spontaneously hypertensive rats

Evidence that blood pressure reduction by serotonin antagonists is related to alpha receptor blockade in spontaneously hypertensive rats. Cohen, Marlene L.; Fuller, Ray W.; Kurz, Ken D. (Lilly Res. Lab., Eli Lilly and Co., Indianapolis, IN 46285, USA). Hypertension (Dallas), 5(5), 676-81 (English) 1983. CODEN: HPRTDN. ISSN: 0194-911X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) In vitro affinity for vascular serotonin (5HT2) and a-receptors was detd. for several compds. (spiperone [749-02-0], ketanserin [74050-98-9], mianserin [24219-97-4], trazodone [19794-93-5], mepiprazole [20326-12-9], benzoctamine [17243-39-9], m-trifluoromethylphenylpiperazine [15532-75-9], m-chlorophenylpiperazine [6640-24-0], and 1-(1-naphthyl)piperazine) [57536-86-4] known to interact with serotonin receptors. All compds. competitively inhibited 5HT2 and a-receptors with differing degrees of selectivity. Based on these observations, ketanserin, benzooctamine, and 1-(1-naphthyl)piperazine were evaluated as antihypertensive agents in spontaneously hypertensive rats (SHR). Of these compds., 1-(1-naphthyl)piperazine was a highly selective 5HT2 receptor antagonist with a ratio of 5HT2 to a-receptor affinity of > 2000. The ratio of 5HT2 to a-receptor affinity for ketanserin and benzoctamine was 63 and 16, resp. However, the order of affinity toward 5HT2 receptors was ketanserin > 1-(1-naphthyl)piperazine > benzoctamine, whereas the order of affinity toward a-receptors was ketanserin > benzoctamine > 1-(1-naphthyl)piperazine. A similar order of potency toward both 5HT2 and a-receptors was found in pithed SHR based on antagonism of the pressor response to serotonin and methoxamine, resp. In the SHR, max. blood pressure redn. at a dose of 10 mg/kg i.p. was approx. 65 and 30 mm Hg for ketanserin and benzooctamine, resp.; 1-(1-naphthyl)piperazine did not affect blood pressure.In this experiment, several chemicals are used like 24219-97-4 and 6640-24-0 Thus, blood pressure redn. more closely paralleled the in vitro and in vivo potency of these agents toward vascular a-rather than 5HT2 receptors. Apparently, a-blockade rather than selective 5HT2 receptor blockade is responsible for the antihypertensive activity of "serotonergic antagonists" in the SHR. .