Characterization of nicotine binding in mouse brain and comparison with the binding of alpha-bungarotoxin and quinuclidinyl benzilate
The binding of (/sup 3/H)nicotine to mouse brain has been measured and subsequently compared with the binding of (/sup 125/I)alpha-bungarotoxin (alpha-BTX) and L-(/sup 3/H)quinuclidinyl benzilate (QNB). The binding of nicotine was saturable, reversible, and stereospecific. Although the rates of association and dissociation of nicotine were temperature-dependent, the incubation temperature had no effect on either KD or Bmax. Nicotine binding was unaffected by the addition of NaCl, KCl, CaCl/sub 2/, or MgSO/sub 4/ to the incubation medium. Nicotinic cholinergic agonists were potent inhibitors of nicotine binding; however, nicotinic antagonists were poor inhibitors. The regional distribution of binding was not uniform: midbrain and striatum contained the highest number of receptors, whereas cerebellum had the fewest. Differences in site densities, regional distribution, inhibitor potencies, and thermal denaturation indicated that nicotine binding was not the same as either QNB or alpha-BTX binding, and therefore that receptors for nicotine may represent a unique population of cholinergic receptors.
- Research Organization:
- Univ. of Colorado, Boulder
- OSTI ID:
- 5764779
- Journal Information:
- Mol. Pharmacol.; (United States), Vol. 22:3
- Country of Publication:
- United States
- Language:
- English
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KINETICS
MICE
PROTEINS
TEMPERATURE DEPENDENCE
TOXINS
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CENTRAL NERVOUS SYSTEM
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HETEROCYCLIC COMPOUNDS
INTERMEDIATE MASS NUCLEI
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MAMMALS
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NUCLEI
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ORGANS
PARASYMPATHOLYTICS
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550601* - Medicine- Unsealed Radionuclides in Diagnostics