The blind mole rat (Spalax ehrenbergi) displays daily and seasonal rhy
thms. Melatonin, secreted nocturnally by the pineal gland, is also pro
duced in the harderian gland and affects its morphology in rodents. We
report here on the presence of putative melatonin receptors in the bl
ind mole rat harderian gland, located in the microsome-enriched fracti
on of the cells. Equilibrium I-125-melatonin binding studies indicated
high- and low-affinity melatonin binding sites in the female (apparen
t Kd 10 pM and 2.4 nM, respectively) and low-affinity sites in the mal
e (apparent Kd 2.6 nM) mole rat. The binding sites were not significan
tly affected by season. Castration increased the density of high-affin
ity binding sites in males and low-affinity binding in females. I-125-
melatonin binding to the gonadectomized mole rat preparation was inhib
ited by serotonin>2-iodomelatonin greater than or equal to memelatonin
>5-methoxytryptamine. The guanine nucleotide analogs, guanosine 5'O-[3
-thio-triphosphate] and guanosine 5'-O-[2-thio-diphosphate], inhibited
specific I-125-melatonin binding, whereas 5'-guanylyl imido-diphospha
te was less potent. These results indicate for the first time the pres
ence of GTP-sensitive melatonin binding sites in the blind mole rat ha
rderian gland, and suggest that their expression is under control of s
ex steroids. (C) 1997 Wiley-Liss, Inc.