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前列腺素受体激动剂和拮抗剂对平滑肌及血小板的作用。

The action of prostanoid receptor agonists and antagonists on smooth muscle and platelets.

作者信息

Eglen R M, Whiting R L

机构信息

Institute of Pharmacology, Syntex Research, Palo Alto, CA 94303.

出版信息

Br J Pharmacol. 1988 Jun;94(2):591-601. doi: 10.1111/j.1476-5381.1988.tb11565.x.

Abstract
  1. Prostanoid receptors have been characterized in a range of guinea-pig and rat smooth muscle and platelets, according to the scheme of Coleman et al., (1985a), using agonists (prostaglandin D2 (PGD2), PGE1, PGE2, 16,16 dimethyl PGE2, PGF2 alpha, PGI2 and U46619) and putative selective antagonists (AH 6809 and SQ 29,548). 2. The ileum possesses EP1- and IP-receptors; the trachea, EP1-EP2- and TP-receptors; the oesophageal muscularis mucosa, EP1- and TP-receptors; the aorta and the portal vein TP-receptors. The rat colon possesses IP-, FP- and TP-receptors. 3. Guinea-pig platelets possess both IP and DP receptors mediating an inhibition of aggregation and TP receptors mediating proaggregation responses. No evidence was found for the presence of EP1-, EP2- or FP-receptors. 4. Misoprostol and fenprostalene were characterized using the above preparations. Misoprostol acts as a selective EP1-agonist, and has little or no DP, FP, IP and TP activity. In the trachea precontracted with carbachol no evidence of EP2-receptor stimulation was observed. Fenprostalene possesses FP and TP activity but no EP1, EP2, DP or IP activity.
摘要
  1. 根据科尔曼等人(1985年a)的方案,使用激动剂(前列腺素D2(PGD2)、前列腺素E1、前列腺素E2、16,16 - 二甲基前列腺素E2、前列腺素F2α、前列环素和U46619)和假定的选择性拮抗剂(AH 6809和SQ 29,548),已在一系列豚鼠和大鼠平滑肌及血小板中对前列腺素受体进行了表征。2. 回肠具有EP1和IP受体;气管具有EP1 - EP2和TP受体;食管肌层黏膜具有EP1和TP受体;主动脉和门静脉具有TP受体。大鼠结肠具有IP、FP和TP受体。3. 豚鼠血小板同时具有介导聚集抑制作用的IP和DP受体以及介导促聚集反应的TP受体。未发现存在EP1、EP2或FP受体的证据。4. 使用上述制剂对米索前列醇和芬前列林进行了表征。米索前列醇作为一种选择性EP1激动剂,几乎没有或没有DP、FP、IP和TP活性。在由卡巴胆碱预收缩的气管中,未观察到EP2受体刺激的证据。芬前列林具有FP和TP活性,但没有EP1、EP2、DP或IP活性。

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