دورية
Pharmacological Characterization of an Epibatidine Binding Site in the Nerve Cord ofPeriplaneta americana
| العنوان: | Pharmacological Characterization of an Epibatidine Binding Site in the Nerve Cord ofPeriplaneta americana |
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| المؤلفون: | Orr, Nailah, Shaffner, Andy J., Watson, Gerald B. |
| المصدر: | Pesticide Biochemistry and Physiology; July 1997, Vol. 58 Issue: 3 p183-192, 10p |
| مستخلص: | A binding site for [3H](±)-epibatidine was found to be present in American cockroach nerve cord homogenates. This binding site was saturable, with aKdof 6.4 ± 0.8 nM and aBmaxof 3.4 ± 1.1 pmol/ mg protein. The pharmacology of this site suggests it to be associated with the nicotinic acetylcholine receptor. (−)-Nicotine, imidacloprid, acetamiprid, (−)-cytisine, and the isomers of epibatidine all displaced [3H](±)-epibatidine. Additionally, all these compounds activated currents from whole-cell patch-clamped cockroach neurons, although there were differences in the magnitudes of maximal currents produced. The nicotinic antagonist, methyllycaconatine, blocked the agonist actions of (−)-nicotine, (+)-epibatidine, and (−)-epibatidine. Methyllycaconatine and α-bungarotoxin also displaced [3H](±)-epibatidine in the cockroach nerve cord homogenates. Attempts at demonstrating specific binding of [3H](±)-epibatidine in house fly head membranes were unsuccessful and may suggest the existence of species-specific epibatidine binding sites or a much lower density of these sites in house fly head membranes. Taken as a whole, the data indicate that [3H](±)-epibatidine labels a site at the nicotinic acetylcholine receptor in cockroach nerve cord and, consequently, should prove useful in the continued characterization of insect nicotinic receptors. |
| قاعدة البيانات: | Supplemental Index |
Full Text Finder | تدمد: | 00483575 10959939 |
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| DOI: | 10.1006/pest.1997.2299 |