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Regulation of m4 muscarinic receptor gene expression

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Selective labeling and localization of the M4 (m4) muscarinic receptor subtype.

Molecular Pharmacology, 1994
We report here a novel strategy for the selective labeling and localization of the M4 (m4) muscarinic receptor subtype, based on the distinct kinetics of the muscarinic antagonists dexetimide and N-methylscopolamine (NMS) and on the selectivity profile of guanylpirenzepine and AF-DX 116 for the m1-m5 muscarinic receptor subtypes expressed in CHO-K1 ...
Ferrari-Dileo, G, Waelbroeck, Magali, Mash, D C, Flynn, D D   +3 more
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Visualization of muscarinic m4 mRNA and M4 receptor subtype in rabbit lung

Life Sciences, 1993
We have used in situ hybridization to study the localization of muscarinic receptor subtype mRNAs and compared this with the distribution of muscarinic receptor subtypes using receptor autoradiography in tissue sections of the rabbit lung. To localize muscarinic receptor subtype mRNAs, subtype-specific synthetic oligonucleotide probes or riboprobes ...
Mak, JCW, Haddad, EB, Buckley, NJ, Barnes, PJ   +3 more
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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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