Muscarinic Cholinergic Binding in Rat Brain

Binding sites with high affinity and specificity for [(3)H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [(3)H]QNB and tissue concentration and is time-, temperature-, and pH-dependent. The bimolecular rate of association (2.0 x 10(8) M(-1) min(-1)) and dissociation (1.2 x 10(-2) min(-1)) at 35 degrees indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [(3)H]QNB binding, while nicotinic and non-cholinergic drugs possess little affinity for [(3)H]QNB-binding sites.