AGONIST-INDUCED AFFINITY ALTERATIONS OF A CENTRAL NERVOUS SYSTEM NICOTINIC ACETYLCHOLINE RECEPTOR

Journal Article · Mon May 01 04:00:00 EDT 1978 · Biochemical and Biophysical Research Communications

OSTI ID:1008319

Lukasiewicz, Ronald J; Bennett, Edward L

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

Related Subjects

99 GENERAL AND MISCELLANEOUS
ACETYLCHOLINE
AFFINITY
BRAIN
CENTRAL NERVOUS SYSTEM
IN VIVO
TOXINS
TRANSFORMATIONS