[3H]cytisine binding to nicotinic cholinergic receptors in brain.
[3H]cytisine binding to nicotinic cholinergic receptors in brain.
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DOI：
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发表时间：
1991
影响因子：
3.6
通讯作者：
L. Pabreza;Subhash Dhawan;K. Kellar
中科院分区：
文献类型：
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作者：
L. Pabreza;Subhash Dhawan;K. Kellar
Cytisine, a ganglionic agonist, competes with high affinity for brain nicotinic cholinergic receptors labeled by any of several nicotinic 3H-agonist ligands. Here we have examined the binding of [3H]cytisine in rat brain homogenates. [3H]Cytisine binds with high affinity (Kd less than 1 nM), and specific binding represented 60-90% of total binding at all concentrations examined up to 15 nM. The nicotinic cholinergic agonists nicotine, acetylcholine, and carbachol compete with high affinity for [3H]cytisine binding sites, whereas among nicotinic receptor antagonists only dihydro-beta-erythroidine competes with high affinity (in the nanomolar range). Comparison of binding in several brain regions showed that [3H]cytisine binding is higher in the thalamus, striatum, and cortex than in the hippocampus, cerebellum, or hypothalamus. The pharmacology and brain regional distribution of [3H]cytisine binding sites are those predicted for neuronal nicotinic receptor agonist recognition sites. The high affinity and low nonspecific binding of [3H]cytisine should make it a very useful ligand for studying neuronal nicotinic receptors.
