Results 211 to 220 of about 8,830 (256)

Investigations into the physiological role of muscarinic M2 and M4 muscarinic and M4 receptor subtypes using receptor knockout mice

Life Sciences, 2001
Determination of muscarinic agonist-induced parasympathomimetic effects in wild type and M2 and M4 muscarinic receptor knockout mice revealed that M2 receptors mediated tremor and hypothermia, but not salivation. The M4 receptors seem to play a modest role in salivation, but did not alter hypothermia and tremor. In the M2 knockout mice, agonist-induced
F P, Bymaster, P A, Carter, L, Zhang, J F, Falcone, P W, Stengel, M L, Cohen, H E, Shannon, J, Gomeza, J, Wess, C C, Felder   +9 more
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Diphenidol-related diamines as novel muscarinic M4 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2008
A series of hydrochloride derivatives 2a-9a and quaternary ammonium derivatives 3b-9b of diphenidol have been synthesized and characterized in receptor binding and cellular functional assays versus human muscarinic M(1)-M(5) receptors expressed in CHO cells.
VAROLI, LUCILLA, ANDREANI, ALDO, BURNELLI, SILVIA, GRANAIOLA, MASSIMILIANO, LEONI, ALBERTO, LOCATELLI, ALESSANDRA, MORIGI, RITA, RAMBALDI, MIRELLA, BEDINI, ANDREA, FAZIO, NICOLA, SPAMPINATO, SANTI MARIO   +10 more
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Characterization of PCS1055, a novel muscarinic M4 receptor antagonist

European Journal of Pharmacology, 2016
Identification of synthetic ligands selective for muscarinic receptor subtypes has been challenging due to the high sequence identity and structural homology among the five muscarinic acetylcholine receptors. Here, we report the pharmacological characterization of PCS1055, a novel muscarinic M4 receptor antagonist.
Carrie H, Croy, Wai Y, Chan, Andrea M, Castetter, Marla L, Watt, Anne T, Quets, Christian C, Felder   +5 more
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Muscarinic m4 receptor activation by some atypical antipsychotic drugs

European Journal of Pharmacology, 1997
To clarify the findings that clozapine is both a muscarinic receptor agonist and antagonist, we examined the effects of neuroleptics on forskolin-stimulated cAMP accumulation in Chinese hamster ovary cells expressing human muscarinic m4 receptors (CHO-hm4) and in rat striatum. With CHO-hm4 cells, clozapine induced a concentration-dependent and atropine-
X P, Zeng, F, Le, E, Richelson
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The M4 muscarinic receptor-selective effects on keratinocyte crawling locomotion

Life Sciences, 2003
We have investigated how the cholinergic system of epidermal keratinocytes (KC) controls migratory function of these cells. Several molecular subtypes of muscarinic acetylcholine receptors (mAChRs) have been detected in KC. Early results suggested that M(4) is the predominant mAChR regulating cell motility.
Alex I, Chernyavsky, Vu Thuong, Nguyen, Juan, Arredondo, Assane, Ndoye, Shaheen, Zia, Jürgen, Wess, Sergei A, Grando   +6 more
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Clozapine is a potent and selective muscarinic M4 receptor agonist

European Journal of Pharmacology: Molecular Pharmacology, 1994
Clozapine was studied in functional assays at human muscarinic M1-M5 receptors expressed in Chinese hamster ovary cells. Clozapine was a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation.
S H, Zorn, S B, Jones, K M, Ward, D R, Liston   +3 more
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Loss of muscarinic M4 receptors in hippocampus of Alzheimer patients

Brain Research, 2003
We assessed muscarinic M(1), M(2) and M(4) receptor subtypes in the hippocampus of Alzheimer's and control brains by receptor autoradiography using ligands such as [(125)I]muscarinic toxin-1 ([(125)I]MT-1, M(1) selective), [(3)H]AFDX-384 (M(2) partially selective) and [(125)I]muscarinic toxin 4 ([(125)I]M(4) toxin-1, M(4) selective).
Mulugeta E, Karlsson E, Islam A, Kalaria R, Mangat H, Winblad B, Adem A   +6 more
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Clozapine interaction with the M2 and M4 subtypes of muscarinic receptors

European Journal of Pharmacology, 1999
Available evidence indicates that the antipsychotic drug clozapine acts as a partial agonist at the muscarinic M4 and as an antagonist at the M2 receptors. We wondered whether there is indeed a fundamental difference between its action on these two receptor subtypes, and whether it interacts with their classical or allosteric binding sites.
P, Michal, M, Lysíková, E E, El-Fakahany, S, Tucek   +3 more
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Muscarinic M4 receptors regulate GABAergic transmission in rat tuberomammillary nucleus neurons

Neuropharmacology, 2012
Histaminergic neurons within the tuberomammillary nucleus (TMN) play an important role in sleep-wakefulness regulation. Here, we report the muscarinic modulation of GABAergic spontaneous miniature inhibitory postsynaptic currents (mIPSCs) in mechanically dissociated rat histaminergic neurons using a conventional whole-cell patch clamp technique ...
Michiko, Nakamura, Il-Sung, Jang
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Muscarinic toxin selective for m4 receptors impairs memory in the rat

NeuroReport, 1998
The selectivity of the muscarinic toxin MT3 from green mamba snake venom was corroborated by inhibition of the binding of [3H]NMS, a classical muscarinic radioligand, to native and cloned muscarinic receptors, showing 214-fold higher affinity for m4 than for m1 subtype, without significant binding to the others. The highest concentrations of MT3 sites (
D, Jerusalinsky, E, Kornisiuk, P, Alfaro, J, Quillfeldt, M, Alonso, E R, Verde, C, Cerveñansky, A, Harvey   +7 more
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