Action of cholinergic drugs on accumulation of TPMP+ on human spermatozoa.

Neurotransmitters or antagonists with nicotinic- or acetylcholine-type receptors were utilized to measure the accumulation of the radiolabeled lipophilic cation triphenylmethylphosphonium (TPMP+) on the plasma membrane of human sperm. Washed sperm incubated in the presence of TPMP+ in a low-K+ or high-K+ medium were allowed to take up the cation to a steady state (i.e., 20 min at 37 degrees C). The difference between TPMP+ in each incubation medium was inserted in the Nernst equation yielding a resting membrane potential of -69 +/- 2 mV. The addition of nicotine or acetylcholine to the low-K+ and high-K+ medium induced a hyperpolarization of 17% and 20%, respectively. In the presence of propranolol the membrane potential decreased by 44%. The association of nicotinic or acetylcholine receptor on human sperm or adrenergic beta-receptor blocking agent may alter the ionic permeability of the membrane, possibly due to hyperpolarization or depolarization.