Shen M R, Linden J, Chiang P H, Chen S S, Wu S N
Graduate Institute of Medicine, Kaohsiung Medical College, Taiwan, R.O.C.
J Pharm Pharmacol. 1993 Jul;45(7):650-3. doi: 10.1111/j.2042-7158.1993.tb05671.x.
The effects of adenosine and its analogues on human sperm motility were studied using a transmembrane migration method. Specific binding sites for adenosine in human sperm were also investigated. Adenosine and 5'-N-ethylcarboxamidoadenosine (NECA) stimulated human sperm motility with similar efficacies and the maximal amplitudes of motility increases were both about 70%. 3,7-Dimethyl-1-propargylxanthine (DMPX), a potent A2 antagonist, competitively antagonized NECA-induced motility stimulation. Successively higher concentrations of DMPX shifted the dose-response curve of NECA to the right in a nearly parallel fashion. Dipyridamole, an inhibitor of adenosine uptake, does not reduce the ability of adenosine to stimulate human sperm motility. In radioligand-binding studies, adenosine A1 selective analogues, cyclopentyl-1,3-dipropylxanthine and 1-methyl-2-phenylethyl adenosine, have little competitive effect on [3H]NECA binding in human sperm membrane. These results provide evidence that adenosine enhances human sperm motility via adenosine A2 receptors on the surface of sperm membranes.
采用跨膜迁移法研究了腺苷及其类似物对人类精子活力的影响。还研究了人类精子中腺苷的特异性结合位点。腺苷和5'-N-乙基羧酰胺腺苷（NECA）以相似的效力刺激人类精子活力，活力增加的最大幅度均约为70%。强效A2拮抗剂3,7-二甲基-1-炔丙基黄嘌呤（DMPX）竞争性拮抗NECA诱导的活力刺激。依次增加DMPX的浓度会使NECA的剂量反应曲线几乎平行地向右移动。腺苷摄取抑制剂双嘧达莫不会降低腺苷刺激人类精子活力的能力。在放射性配体结合研究中，腺苷A1选择性类似物环戊基-1,3-二丙基黄嘌呤和1-甲基-2-苯乙基腺苷对人精子膜中[3H]NECA结合几乎没有竞争作用。这些结果证明腺苷通过精子膜表面的腺苷A2受体增强人类精子活力。
