The effects of adenosine and its analogues on human sperm motility wer
e studied using a transmembrane migration method. Specific binding sit
es 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 increas
es were both about 70%. 3,7-Dimethyl-1-propargylxanthine (DMPX), a pot
ent A2 antagonist, competitively antagonized NECA-induced motility sti
mulation. Successively higher concentrations of DMPX shifted the dose-
response curve of NECA to the right in a nearly parallel fashion. Dipy
ridamole, an inhibitor of adenosine uptake, does not reduce the abilit
y of adenosine to stimulate human sperm motility. In radioligand-bindi
ng studies, adenosine A1 selective analogues, cyclopentyl-1,3-dipropyl
xanthine and 1-methyl-2-phenylethyl adenosine, have little competitive
effect on [H-3]NECA binding in human sperm membrane. These results pr
ovide evidence that adenosine enhances human sperm motility via adenos
ine A2 receptors on the surface of sperm membranes.