蒎烷血栓素A2类似物在大鼠和人胃肌中是非选择性类前列腺素拮抗剂。
Pinane thromboxane A2 analogues are non-selective prostanoid antagonists in rat and human stomach muscle.
作者信息
Bennett A, Sanger G J
出版信息
Br J Pharmacol. 1982 Dec;77(4):591-6. doi: 10.1111/j.1476-5381.1982.tb09336.x.
Abstract
1 Pinane thromboxane A2 (PTxA2) and its epi-OH isomer were studied on rat and human stomach longitudinal muscle. 2 PTxA2 (0.5 micrograms/ml) usually caused a slight contraction of rat gastric fundus. Contractions to PGE2, PGF2 alpha, PGI2 and epoxymethano analogues of PGH2 (U-46619 and U-44069) were substantially inhibited, whereas those to PGD2 and acetylcholine were only slightly reduced. 3 In human stomach, PTxA2 0.5 micrograms/ml rarely stimulated the muscle. Contractions to PGE2, PGF2 alpha and U-46619 were antagonized, with little effect on those to acetylcholine. 4 epi-PTxA2 (0.5 micrograms/ml) did not affect rat gastric tone. It was moderately potent against PGI2 on rat gastric fundus, but was less effective than PTxA2 against U-44069.
摘要
- 对大鼠和人胃纵行肌研究了蒎烷血栓素A2（PTxA2）及其表位-OH异构体。2. PTxA2（0.5微克/毫升）通常引起大鼠胃底轻度收缩。对PGE2、PGF2α、PGI2以及PGH2的环氧甲叉类似物（U-46619和U-44069）的收缩反应被显著抑制，而对PGD2和乙酰胆碱的收缩反应仅略有降低。3. 在人胃中，0.5微克/毫升的PTxA2很少刺激肌肉。对PGE2、PGF2α和U-46619的收缩反应被拮抗，对乙酰胆碱的收缩反应影响很小。4. 表位-PTxA2（0.5微克/毫升）不影响大鼠胃张力。它对大鼠胃底的PGI2有中等强度的作用，但对U-44069的作用比PTxA2弱。
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