Literature DB >> 9346340

Novel persistent activation of muscarinic M1 receptors by xanomeline.

A Christopoulos1, E E El-Fakahany.   

Abstract

The muscarinic agonists, xanomeline and carbachol, displayed similar intrinsic activities in stimulating neuronal nitric oxide synthase at muscarinic M1 receptors in Chinese hamster ovary (CHO) cells, with xanomeline being more potent. Pre-incubation (1 h) with 1 microM xanomeline, followed by extensive washing, resulted in a significantly elevated basal response, which was absent on co-incubation with atropine. This phenomenon was not observed with carbachol. This is the first report of a persistent, receptor-activating effect of a muscarinic agonist.

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Year:  1997        PMID： 9346340     DOI： 10.1016/s0014-2999(97)01162-x

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  6 in total

1.  Long-term wash-resistant effects of brief interaction of xanomeline at the M1 muscarinic receptor.

Authors:  Kayla C De Lorme; Krista L Sikorski; Marianne K O Grant; Esam E El-Fakahany
Journal:  Neurosci Lett       Date:  2006-10-18       Impact factor: 3.046

2.  Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry.

Authors:  M D Wood; K L Murkitt; M Ho; J M Watson; F Brown; A J Hunter; D N Middlemiss
Journal:  Br J Pharmacol       Date:  1999-04       Impact factor: 8.739

3.  Immediate and delayed consequences of xanomeline wash-resistant binding at the M3 muscarinic receptor.

Authors:  Meredith J Noetzel; Marianne K O Grant; Esam E El-Fakahany
Journal:  Neurochem Res       Date:  2008-12-12       Impact factor: 3.996

4.  Pharmacological evaluation of the long-term effects of xanomeline on the M(1) muscarinic acetylcholine receptor.

Authors:  Marianne K O Grant; Meredith J Noetzel; Kayla C De Lorme; Jan Jakubík; Vladimír Doležal; Esam E El-Fakahany
Journal:  PLoS One       Date:  2010-12-23       Impact factor: 3.240

5.  On homology modeling of the M₂ muscarinic acetylcholine receptor subtype.

Authors:  Jan Jakubík; Alena Randáková; Vladimír Doležal
Journal:  J Comput Aided Mol Des       Date:  2013-06-28       Impact factor: 3.686

6.  Long-term activation upon brief exposure to xanomleline is unique to M1 and M4 subtypes of muscarinic acetylcholine receptors.

Authors:  Eva Šantrůčková; Vladimír Doležal; Esam E El-Fakahany; Jan Jakubík
Journal:  PLoS One       Date:  2014-02-18       Impact factor: 3.240
  6 in total

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