The pineal hormone melatonin was found to produce two distinct contrac
tile responses in vascular smooth muscle. In isolated rat caudal arter
y segments, denuded of endothelium, melatonin (10(-10)-10(-7) M) poten
tiated phenylephrine-induced contractions in a concentration-dependent
manner. At higher melatonin concentrations (10(-7)-10(-5) M). however
, the potentiating effect was attenuated. In the presence of the melat
onin MT2 receptor antagonist, 4-phenyl-2-acetamidotetraline (4P-ADOT),
the attenuated constrictor responses were selectively enhanced. These
results are consistent with the hypothesis that melatonin activates t
wo receptor subtypes in vascular smooth muscle; MT2 receptors may indu
ce relaxation, while a second receptor subtype mediates vasoconstricti
on. (C) 1998 Elsevier Science B.V.