Results 221 to 230 of about 58,465 (248)

Identification and Characterization of m1 Selective Muscarinic Receptor Antagonists

Journal of Medicinal Chemistry, 1999
A series of esters of 1,4-disubstituted tetrahydropyridine carboxylic acids (I) has been synthesized and characterized as potential m1 selective muscarinic receptor antagonists. The affinity of these compounds for the five human muscarinic receptor subtypes (Hm1-Hm5) was determined by the displacement of [3H]-NMS binding using membranes from ...
Roy D. Schwarz, C.B. Nelson, Anthony Jerome Thomas, C. J. Blankley, Penvose-Yi, C.E. Augelli-Szafran, D.W. Moreland, Juan C. Jaen   +7 more
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M1 and M3 muscarinic receptors

NeuroReport, 1992
P-fluoro-hexahydro-sila-difenidol hydrochloride (p-F-HHSiD) (15, 30 micrograms) and pirenzepine (7.5, 15, 30 micrograms), which are highly selective M3 and M1 muscarinic antagonists, respectively, were injected intracerebroventricularly into freely moving rats.
L. IMERI, S. BIANCHI, P. ANGELI, M. MANCIA   +3 more
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M1 Receptor Agonist Activity Is Not a Requirement for Muscarinic Antinociception

The Journal of Pharmacology and Experimental Therapeutics, 1997
The analgesic effects of a series of muscarinic agonists were investigated by use of the mouse acetic acid writhing, grid-shock, hot-plate and tail-flick tests. The compounds tested were oxotremorine, pilocarpine, arecoline, aceclidine, RS86 and four 3-3(substituted-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahy-dro-1 -methyl pyridines (substituted TZTP ...
M J, Sheardown, H E, Shannon, M D, Swedberg, P D, Suzdak, F P, Bymaster, P H, Olesen, C H, Mitch, J S, Ward, P, Sauerberg   +8 more
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Is the effect of somatostatin on muscarinic receptors selective to M1 type?

Brain Research, 1986
The effect of somatostatin on muscarinic receptors (mAchR) was investigated through saturation experiments of [3H]oxotremorine-M-acetate and oxotremorine/[3H]N-methyl-scopolamine competition experiments. Somatostatin converted oxotremorine high affinity binding sites to low affinity sites in the hippocampus and cerebral cortex whose mAchR were ...
Rie Miyoshi, Shozo Kito, Hiroaki Matsubayashi, Kumiko Mizuno   +3 more
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Characterization of M1- and M2-muscarinic receptors in calf retina membranes

Vision Research, 1988
Muscarinic receptors are identified in bovine retina membranes by the specific binding of 1-[benzilic-4,4'-3H]-quinuclidinyl benzilate [3H]-QNB. Binding occurs to one population of non-cooperative binding sites: KD = 0.11 +/- 0.02 nM and Bmax = 0.61 +/- 0.07 pmol/mg protein.
Vanderheyden, P, Ebinger, G, Vauquelin, G   +2 more
openaire   +4 more sources

Targeting of Diacylglycerol Degradation to M1 Muscarinic Receptors by ß-Arrestins

Science, 2007
Seven-transmembrane receptor (7TMR) signaling is transduced by second messengers such as diacylglycerol (DAG) generated in response to the heterotrimeric guanine nucleotide–binding protein G q and is terminated by receptor desensitization and degradation of the second messengers.
Christopher D. Nelson, Debra S. Regier, Stephen M. Prescott, Matthew K. Topham, Stephen J. Perry, Robert J. Lefkowitz, Robert J. Lefkowitz   +6 more
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Allosteric regulation of cloned m1–m5 muscarinic receptor subtypes

Biochemical Pharmacology, 1991
Allosteric regulation of [3H]N-methylscopolamine [( 3H]NMS) and [3H]quinuclidinyl benzilate [( 3H]QNB) dissociation from the m1-m5 muscarinic receptor subtypes was examined in transfected CHO-K1 cells. Half-times of dissociation of [3H]NMS from cell membranes (at 23 degrees) ranged from less than 5 min for the m2 subtype to more than 60 min for the m5 ...
John Ellis, Mark R. Brann, Mark R. Brann, Joanne H. Huyler   +3 more
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Astrocytes have both M1 and M2 muscarinic receptor subtypes

Brain Research, 1986
In astrocytes, carbachol evoked the turnover of membrane inositol phospholipids prelabelled with [3H]inositol, as revealed by [3H]inositol phosphate accumulation in the presence of 5 mM lithium. This effect was blocked by atropine and by pirenzepine (IC50 2.2 nM and 56 nM, respectively).
Christine Morrow, Brian Pearce, Sean Murphy   +2 more
openaire   +3 more sources

Involvement of M1-muscarinic receptors in the excitation of neocortical neurones by acetylcholine

Neuropharmacology, 1987
The technique of microelectrophoresis was used to investigate the cholinoceptor pharmacology of spontaneously active single neurones in the parietal cortex of the rat. Acetylcholine, carbachol and the selective M1-muscarinic receptor agonist, McN-A-343, were each potent excitants (rank order of apparent potency: carbachol greater than acetylcholine ...
C. M. Bradshaw, R.D. Sheridan, E. Szabadi   +2 more
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Autoradiographic localization of M1 and M2 muscarine receptors in the rat brain

Neuroscience, 1986
The distribution of M1 and M2 muscarine receptors in the rat brain was investigated by in vitro autoradiography. Muscarine receptors were visualized after complete receptor uncoupling in ethylenediaminetetraacetic acid buffer containing 1 mM N-ethyl maleimide and saturation with the ligand [3H]quinuclidinyl benzilate.
L.T. Potter, D.C. Mash
openaire   +3 more sources