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Received for publication May 10, 2004.
Revised June 25, 2004.
Accepted for publication July 8, 2004.
3 
4 Subtype
The rat pineal gland contains a high density of neuronal nicotinic receptors (nAChRs). We characterized the pharmacology of the binding sites and function of these receptors, measured the nAChR subunit mRNA and used subunit-specific antibodies to establish the receptor subtype as defined by subunit composition. In ligand binding studies, [3H]epibatidine binds with an affinity of
100 pM to nAChRs in the pineal, and the density of these sites is 5-times that in rat cerebral cortex. The affinities of nicotinic drugs for binding sites in the pineal gland are similar to those at 
3 
4 nAChRs heterologously expressed in HEK293 cells. In functional studies, the potencies and efficacies of nicotinic drugs to activate or block whole cell currents in dissociated pinealocytes match closely their potencies and efficacies to activate or block 86Rb+ efflux in the cells expressing heterologous 3 4 nAChRs. Measurements of mRNA indicated the presence of transcripts for 3, 2 and 4 nAChR subunits but not those for 2, 4, 5, 6, 7, or 3 subunits. Immunoprecipitation with subunit-specific antibodies showed that virtually all [3H]EB-labeled nAChRs contained 3 and 4 subunits associated in one complex. The 2 subunit was not associated with this complex. Taken together, these results indicate that virtually all of the nAChRs in the rat pineal gland are the 3 4 nAChR subtype, and that the pineal gland can therefore serve as an excellent and convenient model in which to study the pharmacology and function of these receptors in a native tissue
Key words:
Nicotinic cholinergic, Receptor binding studies
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