Abstract
Using radiolabeled 2-iodomelatonin ([125I]-labeled melatonin, 125I-MEL; Vakkuri et al., 1984), a potent melatonin agonist (Weaver et al., 1988), high-affinity melatonin binding sites have recently been characterized in a number of tissues by several different laboratories. High-affinity sites have equilibrium dissociation constants (Kd values) ≤ 200 pM at room temperature; Kd values in most reports are ca 40 pM. High-affinity melatonin binding sites have been demonstrated in avian, reptilian, and mammalian tissues (Dubocovich & Takahashi, 1987; Rivkees et al., 1989a; Vanecek et al., 1987; Duncan et al., 1989; Carlson et al., 1989; Weaver et al., 1989; Morgan et al., 1989c). The pharmacologic specificity of the high-affinity sites identified in these various tissues is generally in good agreement.
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Reppert, S.M., Weaver, D.R., Rivkees, S.A. (1991). High-Affinity Melatonin Receptors in Mammals: Localization, G-Protein Coupling and Signal Transduction. In: Fraschini, F., Reiter, R.J. (eds) Role of Melatonin and Pineal Peptides in Neuroimmunomodulation. NATO ASI Series, vol 204. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-3756-4_9
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