Bodelsson M, Törnebrandt K, Bertilsson I L, Arneklo-Nobin B
Department of Anaesthesiology, Lund University, Sweden.
Eur J Pharmacol. 1992 Sep 4;219(3):455-60. doi: 10.1016/0014-2999(92)90488-p.
To increase our knowledge of human peripheral vasospasm we characterized the contractile 5-hydroxytryptamine (5-HT) receptors in human superficial hand vein segments in vitro. The 5-HT1 receptor agonist, sumatriptan, the 5-HT2 receptor agonist, dl-alpha-methyl-5-HT, and the 5-HT3 receptor agonist, 2-methyl-5-HT, all induced concentration-dependent contractions. The contractile response to sumatriptan was antagonized by the non-selective 5-HT receptor antagonist, methiothepin, but was unaffected by the 5-HT2 receptor antagonist, ketanserin. The contractile response to dl-alpha-methyl-5-HT was antagonized by both methiothepin and ketanserin. The contraction elicited by 2-methyl-5-HT was not affected by the 5-HT3 receptor antagonist, MDL 72222, but was antagonized by ketanserin. The results suggest that serotonergic contraction in the human superficial hand vein involves both 5-HT1 and 5-HT2 but not 5-HT3 receptors. Such receptor heterogeneity in human blood vessels should be considered when using drugs and when designing future compounds for medical use.
为增加我们对人类外周血管痉挛的了解,我们在体外对人手部浅静脉段中的收缩性5-羟色胺(5-HT)受体进行了表征。5-HT1受体激动剂舒马曲坦、5-HT2受体激动剂dl-α-甲基-5-HT和5-HT3受体激动剂2-甲基-5-HT均诱导浓度依赖性收缩。对舒马曲坦的收缩反应被非选择性5-HT受体拮抗剂美噻吨拮抗,但不受5-HT2受体拮抗剂酮色林影响。对dl-α-甲基-5-HT的收缩反应被美噻吨和酮色林均拮抗。2-甲基-5-HT引发的收缩不受5-HT3受体拮抗剂MDL 72222影响,但被酮色林拮抗。结果表明,人手部浅静脉中的5-羟色胺能收缩涉及5-HT1和5-HT2受体,但不涉及5-HT3受体。在使用药物以及设计未来医用化合物时,应考虑人类血管中的这种受体异质性。