AGONIST-INDUCED AFFINITY ALTERATIONS OF A CENTRAL NERVOUS SYSTEM NICOTINIC ACETYLCHOLINE RECEPTOR
Pretreatment of {alpha}-bungarotoxin ({alpha}-Bgt) binding sites from rat brain with cholinergic agonists causes transformation of sites to a high-affinity form toward agonist over a time course of minutes, consistent with identity of those sites as central nicotinic acetylcholine receptors (nAChR). This agonist-induced alteration in receptor state may be correlated with physiological densensitization. Agonist inhibition of toxin binding to the high-affinity state is non-competitive, suggesting the existence of discrete toxin-binding and agonist-binding sites on the central nAChR. These results thus offer a possible explanation of observed impotency of {alpha}-Bgt toward blocking in vivo cholinergic responses in the central nervous system.
- Research Organization:
- Ernest Orlando Lawrence Berkeley National Laboratory, Berkeley, CA (US)
- Sponsoring Organization:
- Chemical Sciences Division
- DOE Contract Number:
- AC02-05CH11231
- OSTI ID:
- 1008319
- Report Number(s):
- LBL-7594
- Journal Information:
- Biochemical and Biophysical Research Communications, Journal Name: Biochemical and Biophysical Research Communications; ISSN BBRCA9; ISSN 0006-291X
- Country of Publication:
- United States
- Language:
- English
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