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Differentiation of muscarinic cholinergic receptor subtypes in human cortex and pons - Implications for anti-motion sickness therapyRadioligand binding studies were used to analyze muscarinic cholinergic receptor subtypes in human cortex and pons. Muscarinic cholinergic receptors were labeled by H-3-quinuclidinyl benzilate (H-3-QNB). Scopolamine was equipotent in both brain regions and did not discriminate subtypes of H-3-QNB binding. By contrast, the M1 selective antagonist pirenzepine was approximately 33-fold more potent in human cortex than pons. Carbachol, a putative M2 selective agonist, was more than 100-fold more potent in human pons than cortex. These results demonstrate that the human pons contains a relatively large proportion of carbachol-sensitive muscarinic cholinergic receptors. Drugs targeted to this subpopulation of muscarinic cholinergic receptors may prove to be effective anti-motion sickness agents with less side effects than scopolamine.
Document ID
19880037321
Acquisition Source
Legacy CDMS
Document Type
Reprint (Version printed in journal)
Authors
Mccarthy, Bruce G.
(Stanford Univ. CA, United States)
Peroutka, Stephen J.
(Stanford University, Medical Center CA, United States)
Date Acquired
August 13, 2013
Publication Date
January 1, 1988
Publication Information
Publication: Aviation, Space, and Environmental Medicine
Volume: 59
ISSN: 0095-6562
Subject Category
Aerospace Medicine
Accession Number
88A24548
Funding Number(s)
CONTRACT_GRANT: NCA2-IR-745-504
Distribution Limits
Public
Copyright
Other

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