Putative melatonin receptors in the blind mole rat harderian gland

The blind mole rat (Spalax ehrenbergi) displays daily and seasonal rhythms. Melatonin, secreted nocturnally by the pineal gland, is also produced in the harderian gland and affects its morphology in rodents. We report here on the presence of putative melatonin receptors in the blind mole rat harderian gland, located in the microsome-enriched fraction of the cells. Equilibrium ¹²⁵I-melatonin binding studies indicated high- and low-affinity melatonin binding sites in the female (apparent Kd 10 pM and 2.4 nM, respectively) and low-affinity sites in the male (apparent Kd 2.6 nM) mole rat. The binding sites were not significantly affected by season. Castration increased the density of high-affinity binding sites in males and low-affinity binding in females. ¹²⁵I-melatonin binding to the gonadectomized mole rat preparation was inhibited by serotonin>2-iodomelatonin≤memelatonin>5-methoxytryptamine. The guanine nucleotide analogs, guanosine 5'-O-[3-thio-triphosphate] and guanosine 5'-O-[2-thio-diphosphate], inhibited specific ¹²⁵I-melatonin binding, whereas 5'-guanylyl imido-diphosphate was less potent. These results indicate for the first time the presence of GTP-sensitive melatonin binding sites in the blind mole rat harderian gland, and suggest that their expression is under control of sex steroids.