Pinane Thromboxane A2 Analogues Are Non-selective Prostanoid Antagonists in Rat and Human Stomach Muscle
Overview
Authors
Affiliations
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.
Xu K, Shimizu M, Murai C, Fujisawa M, Ito D, Saitoh N Pharmacol Res Perspect. 2022; 10(3):e00952.
PMID: 35466586 PMC: 9035583. DOI: 10.1002/prp2.952.
Kim J, Choi S, Yeum C, Yoon P, Choi S, Jun J Korean J Physiol Pharmacol. 2010; 12(1):25-30.
PMID: 20157390 PMC: 2817529. DOI: 10.4196/kjpp.2008.12.1.25.
Okada Y, Hara A, Ma H, Xiao C, Takahata O, Kohgo Y Br J Pharmacol. 2000; 131(4):745-55.
PMID: 11030724 PMC: 1572385. DOI: 10.1038/sj.bjp.0703627.
Prostaglandin D2 interacts at thromboxane receptor-sites on guinea-pig platelets.
Whittle B Br J Pharmacol. 1986; 88(4):931-6.
PMID: 3017497 PMC: 1917072. DOI: 10.1111/j.1476-5381.1986.tb16268.x.