Whiteaker_2000_Eur.J.Pharmacol_393_123

Reference

Title : Pharmacological and null mutation approaches reveal nicotinic receptor diversity - Whiteaker_2000_Eur.J.Pharmacol_393_123
Author(s) : Whiteaker P , Marks MJ , Grady SR , Lu Y , Picciotto MR , Changeux JP , Collins AC
Ref : European Journal of Pharmacology , 393 :123 , 2000
Abstract :

We have developed an array of assays for nicotinic acetylcholine receptor binding and function. [125I]alpha-Bungarotoxin-, (-)-[3H]nicotine-, and [3H]epibatidine-binding nicotinic acetylcholine receptors were assayed in mouse brain membranes and sections. Nicotinic acetylcholine receptor function was quantified using synaptosomal [3H]dopamine, [3H]gamma-aminobutyric acid ([3H]GABA), and 86Rb(+) efflux techniques. Additionally, the effects of beta2 subunit deletion on each of the measures were assessed. Detailed pharmacological comparison revealed minimally six nicotinic binding subtypes: [125I]alpha-bungarotoxin-binding nicotinic acetylcholine receptors; beta2-subunit-dependent and -independent high-affinity (-)-[3H]nicotine-binding sites; beta2-dependent and -independent cytisine-resistant [3H]epibatidine-binding sites; and a beta2-dependent low-affinity [3H]epibatidine binding site. Comparative pharmacology suggested that [3H]GABA and dihydro-beta-erythroidine (DHbetaE)-sensitive 86Rb(+) efflux are mediated by the same (probably alpha4beta2) nicotinic acetylcholine receptor subtype, while other nicotinic acetylcholine receptor subtypes evoke [3H]dopamine and DHbetaE-resistant 86Rb(+) efflux. In whole-brain preparations, each measure of nicotinic acetylcholine receptor function was beta2 dependent. The majority of beta2-independent [3H]epibatidine binding was located in small, scattered brain nuclei, suggesting that individual nuclei may prove suitable for identification of novel, native nicotinic acetylcholine receptors.

PubMedSearch : Whiteaker_2000_Eur.J.Pharmacol_393_123
PubMedID: 10771005

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Citations formats

Whiteaker P, Marks MJ, Grady SR, Lu Y, Picciotto MR, Changeux JP, Collins AC (2000)
Pharmacological and null mutation approaches reveal nicotinic receptor diversity
European Journal of Pharmacology 393 :123

Whiteaker P, Marks MJ, Grady SR, Lu Y, Picciotto MR, Changeux JP, Collins AC (2000)
European Journal of Pharmacology 393 :123