Burnstock G, Cusack N J, Meldrum L A
Br J Pharmacol. 1984 Jun;82(2):369-74. doi: 10.1111/j.1476-5381.1984.tb10771.x.
Phosphorothioate analogues of ATP, ADP and AMP were tested on the guinea-pig taenia coli and urinary bladder. The Rp diastereoisomers of the phosphorothioate analogues, ATP-alpha-S and ADP-alpha-S were respectively 7 and 3 times more effective than the Sp diastereoisomers in causing relaxation of the taenia coli. No stereoselectivity was observed for the diastereoisomers of ATP-beta-S. In guinea-pig bladder, no stereoselectivity was observed for any of the phosphorothioate analogues. These results show that P2-purinoceptors mediating inhibitory responses in the guinea-pig taenia coli show marked stereoselectivity, while P2-purinoceptors mediating excitatory responses in the guinea-pig bladder show little stereoselectivity.
对ATP、ADP和AMP的硫代磷酸酯类似物在豚鼠结肠带和膀胱上进行了测试。硫代磷酸酯类似物ATP-α-S和ADP-α-S的Rp非对映异构体在引起结肠带松弛方面分别比Sp非对映异构体有效7倍和3倍。对于ATP-β-S的非对映异构体未观察到立体选择性。在豚鼠膀胱中,对任何硫代磷酸酯类似物均未观察到立体选择性。这些结果表明,介导豚鼠结肠带抑制性反应的P2嘌呤受体表现出明显的立体选择性,而介导豚鼠膀胱兴奋性反应的P2嘌呤受体几乎没有立体选择性。