Muscarinic cholinergic binding in rat brain

H. I. Yamamura; S. H. Snyder

doi:10.1073/pnas.71.5.1725

Muscarinic cholinergic binding in rat brain

H. I. Yamamura, S. H. Snyder

School of Medicine

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1233 Scopus citations

Abstract

Binding sites with high affinity and specificity for [³H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [³H]QNB and tissue concentration and is time, temperature, and pH dependent. The bimolecular rate of association (2.0 x 10⁸ M^-1 min^-1) and dissociation (1.2 x 10^-2 min^-1) at 35°C indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [³H]QNB binding, while nicotinic and noncholinergic drugs possess little affinity for [³H]QNB binding sites.

Original language	English (US)
Pages (from-to)	1725-1729
Number of pages	5
Journal	Proceedings of the National Academy of Sciences of the United States of America
Volume	71
Issue number	5
DOIs	https://doi.org/10.1073/pnas.71.5.1725
State	Published - 1974

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title = "Muscarinic cholinergic binding in rat brain",

abstract = "Binding sites with high affinity and specificity for [3H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [3H]QNB and tissue concentration and is time, temperature, and pH dependent. The bimolecular rate of association (2.0 x 108 M-1 min-1) and dissociation (1.2 x 10-2 min-1) at 35°C indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [3H]QNB binding, while nicotinic and noncholinergic drugs possess little affinity for [3H]QNB binding sites.",

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T1 - Muscarinic cholinergic binding in rat brain

AU - Yamamura, H. I.

AU - Snyder, S. H.

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N2 - Binding sites with high affinity and specificity for [3H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [3H]QNB and tissue concentration and is time, temperature, and pH dependent. The bimolecular rate of association (2.0 x 108 M-1 min-1) and dissociation (1.2 x 10-2 min-1) at 35°C indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [3H]QNB binding, while nicotinic and noncholinergic drugs possess little affinity for [3H]QNB binding sites.

AB - Binding sites with high affinity and specificity for [3H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [3H]QNB and tissue concentration and is time, temperature, and pH dependent. The bimolecular rate of association (2.0 x 108 M-1 min-1) and dissociation (1.2 x 10-2 min-1) at 35°C indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [3H]QNB binding, while nicotinic and noncholinergic drugs possess little affinity for [3H]QNB binding sites.

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Muscarinic cholinergic binding in rat brain

Abstract

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