Results 141 to 150 of about 12,342 (188)

Amplification of the rat m2 muscarinic receptor gene by the polymerase chain reaction: Functional expression of the M2 muscarinic receptor

Life Sciences, 1990
A selective amplification of the coding sequence of the rat M2 muscarinic receptor gene was achieved by the polymerase chain reaction. The error rate of this amplification system under conditions specified was 1 nucleotide substitution in 841 base pairs.
J, Lai, J W, Bloom, H I, Yamamura, W R, Roeske   +3 more
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Evidence of paired M2 muscarinic receptors.

Molecular Pharmacology, 1991
Binding assays involving various antagonists, including N-[3H] methylscopolamine, [3H]quinuclidinyl benzilate, AFDX-116, pirenzepine, and propylbenzilylcholine mustard, disclosed only a single population of M2 muscarinic receptors in membranes from the rat "brainstem" (medulla, pons, and colliculi).
L T, Potter, L A, Ballesteros, L H, Bichajian, C A, Ferrendelli, A, Fisher, H E, Hanchett, R, Zhang   +6 more
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Immunohistochemical localization of muscarinic receptors (M2) in the rat skin

Cell and Tissue Research, 2000
Acetylcholine (ACh) produces pain when applied to human skin and excites cutaneous mechanoreceptors and nerve terminals. These effects are partially mediated by activation of muscarinic receptors. The expression of muscarinic receptor subtype M2 has been shown in sensory neurons of rat dorsal root ganglia using reverse transcriptase polymerase chain ...
R V, Haberberger, M, Bodenbenner
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A novel function of the M2 muscarinic receptor

Trends in Pharmacological Sciences
The M2 muscarinic receptor (M2R) is a prototypic class A G protein-coupled receptor (GPCR). Interestingly, Fasciani et al. recently identified an internal translation start site within the M2 receptor mRNA, directing the expression of a C-terminal receptor fragment.
Jürgen Wess, Liu Liu
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Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor

Bioorganic & Medicinal Chemistry Letters, 2000
Structure activity studies on [4-(phenylsulfonyl)phenyl]methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4-methoxyphenyl(S)-sufinyl]phenyl]-1-pi perazineacetonitrile, 1, an M2 selective muscarinic antagonist. Affinity at the cloned human M2 receptor was 2.7 nM; the M1/M2 selectivity is 40-fold.
J A, Kozlowski, D B, Lowe, H S, Guzik, G, Zhou, V B, Ruperto, R A, Duffy, R, McQuade, G, Crosby, L A, Taylor, W, Billard, H, Binch, J E, Lachowicz   +11 more
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Cholesterol as a determinant of cooperativity in the M2 muscarinic cholinergic receptor

Biochemical Pharmacology, 2007
M2 muscarinic receptor extracted from Sf9 cells in cholate-NaCl differs from that extracted from porcine sarcolemma. The latter has been shown to exhibit an anomalous pattern in which the capacity for N-[3H]methylscopolamine (NMS) is only 50% of that for [3H]quinuclidinylbenzilate (QNB), yet unlabeled NMS exhibits high affinity for all of the sites ...
Alejandro T, Colozo, Paul S-H, Park, Chi Shing, Sum, Luca F, Pisterzi, James W, Wells   +4 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
openaire   +2 more sources

Benzylidene ketal derivatives as M2 muscarinic receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2000
Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition.
C D, Boyle, S, Chackalamannil, L Y, Chen, S, Dugar, P, Pushpavanam, W, Billard, H, Binch, G, Crosby, M, Cohen-Williams, V L, Coffin, R A, Duffy, V, Ruperto, J E, Lachowicz   +12 more
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Interaction of Mg2+ with the allosteric site of muscarinic M2 receptors

Naunyn-Schmiedeberg's Archives of Pharmacology, 1998
Mg2+-ions have been suspected to attenuate the inhibitory effect of allosteric modulators on the dissociation of orthosteric ligands from muscarinic M2 receptors. It was aimed to gain more insight into the molecular events underlying the effect of Mg2+.
U, Burgmer, U, Schulz, C, Tränkle, K, Mohr   +3 more
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Expression of muscarinic receptor subtypes and M2-muscarinic inhibition of adenylyl cyclase in lung

American Journal of Physiology-Lung Cellular and Molecular Physiology, 1995
The relative distribution and absolute quantities of muscarinic receptor subtypes m1, m2, m3, and m4 were determined in membranes of canine trachealis muscle, bronchi, and lung parenchyma by immuno-precipitation with receptor subtype-specific rabbit polyclonal antisera. Additionally, the functional coupling of muscarinic receptors to the inhibition of
C W, Emala, A, Aryana, M A, Levine, R P, Yasuda, S A, Satkus, B B, Wolfe, C A, Hirshman   +6 more
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