Results 141 to 150 of about 15,215 (194)

Interaction Studies of Multiple Binding Sites on M4 Muscarinic Acetylcholine Receptors

Molecular Pharmacology, 2006
This study investigated the reciprocal cross-interactions between two distinct allosteric sites on the M(4) muscarinic acetylcholine receptor (mAChR) in the absence or presence of different orthosteric ligands. Initial studies revealed that two novel benzimidazole allosteric modulators, 17-beta-hydroxy-17-alpha-ethy nyl-delta(4)-androstano[3,2-b ...
Alfred A, Lanzafame, Patrick M, Sexton, Arthur, Christopoulos   +2 more
openaire   +2 more sources

Enhanced self-administration of alcohol in muscarinic acetylcholine M4 receptor knockout mice

European Journal of Pharmacology, 2015
Modulation of cholinergic neurotransmission via nicotinic acetylcholine receptors is known to alter alcohol-drinking behavior. It is not known if muscarinic acetylcholine receptor subtypes have similar effects. The muscarinic M4 receptor is highly expressed in the brain reinforcement system and involved in regulation of cholinergic and dopaminergic ...
de la Cour, Cecilie, Sørensen, Gunnar, Wörtwein, Gitta, Weikop, Pia, Nielsen, Ditte Dencker, Fink-Jensen, Anders, Molander, Anna   +6 more
openaire   +3 more sources

Receptor internalization delays m4 muscarinic acetylcholine receptor resensitization at the plasma membrane.

Molecular Pharmacology, 1996
We analyzed the role of receptor internalization and recycling in muscarinic acetylcholine receptor (mAChR) desensitization and resensitization. Incubation of Chinese hamster ovary cells stably expressing the m4 mAChR with 1 mM carbachol for 1 hr reduced cell surface receptor number by 50-60% with no change in total receptor number. Pretreatment of the
G S, Bogatkewitsch, W, Lenz, K H, Jakobs, C J, Van Koppen   +3 more
openaire   +2 more sources

Elongation Factor 1A Family Regulates the Recycling of the M4 Muscarinic Acetylcholine Receptor

Neurochemical Research, 2006
In this study, we tested the hypothesis that the elongation 1A (eEF1A) family regulates the cell surface density of the M4 subtype of the muscarinic acetylcholine receptors (mAChR) following agonist-induced internalization. Here, we show that mouse brains lacking eEF1A2 have no detectable changes in M4 expression or localization.
Daniel B, McClatchy, Guofu, Fang, Allan I, Levey   +2 more
openaire   +2 more sources

Isolation, sequence and functional expression of the mouse m4 muscarinic acetylcholine receptor gene

Biochimica et Biophysica Acta (BBA) - Gene Structure and Expression, 1993
Molecular cloning studies have demonstrated the existence in mammals of five genes encoding distinct muscarinic acetylcholine receptors which are heterogeneously expressed in the central nervous system and the target organs of the autonomic nervous system.
C J, van Koppen, W, Lenz, N M, Nathanson
openaire   +2 more sources

Human skin fibroblasts express m2, m4, and m5 subtypes of muscarinic acetylcholine receptors

Journal of Cellular Biochemistry, 1999
Previous studies have demonstrated that muscarinic acetylcholine receptors (mAChRs) are expressed by human skin fibroblasts (HSF). We have identified the molecular subtypes of these receptors by reverse transcription-polymerase chain reaction (RT-PCR), using m1-m5 subtype-specific primers.
R, Buchli, A, Ndoye, J G, Rodriguez, S, Zia, R J, Webber, S A, Grando   +5 more
openaire   +2 more sources

The Prosperity and Adversity of M4 Muscarinic Acetylcholine Receptor Activators in the Treatment of Neuropsychiatric Disorders.

Journal of Medicinal Chemistry
Since the serendipitous discovery of chlorpromazine in the 1950s, almost all current anti-schizophrenia drugs utilize the same mode of action by blocking the dopamine receptors in the brain.
Boqun Liu, A. Christopoulos, D. Thal, B. Capuano, C. Valant, P. Scammells   +5 more
semanticscholar   +1 more source

Acetylcholine induces Ca 2+ oscillations via m3/m4 muscarinic receptors in the mouse oocyte

Pfl�gers Archiv European Journal of Physiology, 2003
Changes in intracellular Ca2+ concentration are required for the activation of mammalian oocytes. They are caused mainly by Ca2+ release from the endoplasmic reticulum (ER) via Ins P3 receptors (Ins P3R). Several studies have reported that acetylcholine (ACh) is capable of triggering early activation events in mouse oocytes over-expressed with the m1 ...
Dawon, Kang, Jae-Yong, Park, Jaehee, Han, In-Ha, Bae, Sook-Young, Yoon, Sang Soo, Kang, Wan Sung, Choi, Seong-Geun, Hong   +7 more
openaire   +2 more sources

Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.

Journal of Medicinal Chemistry
Selective activation of the M4 muscarinic acetylcholine receptor subtype offers a novel strategy for the treatment of psychosis in multiple neurological disorders.
Christopher R Butler, M. Popiolek, Laura A McAllister, Erik A. Lachapelle, Melissa Kramer, Elizabeth M Beck, S. Mente, M. Brodney, Matthew Brown, Adam M. Gilbert, Chris Helal, Kevin Ogilvie, Jeremy Starr, Daniel Uccello, Sarah Grimwood, Jeremy R. Edgerton, Jonathan Garst-Orozko, Rouba Kozak, Susan Lotarski, A. Rossi, Deborah Smith, Rebecca O’Connor, J. Lazzaro, C. Steppan, Stefanus J. Steyn   +24 more
semanticscholar   +1 more source

Vinburnine decelerates [3H]N-methylscopolamine binding to recombinant human muscarinic M1–M4 acetylcholine receptors

European Journal of Pharmacology, 2004
The kinetics of [3H]N-methylscopolamine binding to membranes of Chinese hamster ovary (CHO) cells expressing muscarinic M(1)-M(4) acetylcholine receptors was studied. [3H]N-methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-eburnamonine). [3H]N-methylscopolamine dissociation was decelerated
Gábor, Maksay, Tímea, Bíró, Béla, Kiss   +2 more
openaire   +2 more sources