Results 191 to 200 of about 18,745 (209)

Synthesis of antagonists of muscarinic (M3) receptors

Collection of Czechoslovak Chemical Communications, 2011
Several α-hydroxyamides with (2,6-dialkoxyphenoxy)methyl substituents have been prepared and their activities as antagonists of the M3 muscarinic receptor in guinea pig ileum have been evaluated. N-{1-[(Phenyl)methyl]piperidin-4-yl}-2-{2-[(2,6-dimethoxyphenoxy)-methyl]phenyl}-2-hydroxypropanamide and N-(1-[{6-amino-4-[(1-propylpiperidin-4-yl)methyl ...
Broadley, Kenneth J., Davies, Robin H., Escargueil, Christine, Lee, Alan T L, Penson, Peter, Thomas, Eric J.   +5 more
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J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors

Bioorganic & Medicinal Chemistry, 1999
A new class of 4-acetamidopiperidine derivatives has been synthesized and investigated for human muscarinic receptor subtype selectivity. Introduction of a hydrocarbon chain of appropriate length into the piperidine nitrogen of the racemic N-(piperidin-4-yl)-2-cyclobutyl-2-hydroxy-2-phenylacetamide platform conferred up to 70-fold selectivity for human
M, Mitsuya, T, Mase, Y, Tsuchiya, K, Kawakami, H, Hattori, K, Kobayashi, Y, Ogino, T, Fujikawa, A, Satoh, T, Kimura, K, Noguchi, N, Ohtake, K, Tomimoto   +12 more
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Potential Benefits of Muscarinic M3 Receptor Selectivity

European Urology Supplements, 2002
Abstract Detrusor smooth muscle contains muscarinic receptors of the M 2 (≈2/3) and M 3 (≈1/3) subtypes. M 3 receptors are mainly responsible for normal micturition contraction, whereas, the role of M 2 receptors has not yet been clarified. In certain disease states, M 2 receptors may also contribute to bladder contraction.
openaire   +1 more source

Effect of a muscarinic M3 receptor agonist on gastric motility

Journal of Gastroenterology and Hepatology, 2007
AbstractMuscarinic M3 receptors exist in the gastrointestinal wall in humans and the muscarinic M3 agonist cevimeline hydrochloride (Evoxac) is a candidate therapeutic agent for the treatment of xerostomia in Sjögren’s syndrome. However, M3 receptor agonists are not known to show efficacy for diseases associated with abnormal gastrointestinal motility.
Toshimi, Chiba, Norihiko, Kudara, Masaki, Sato, Masaaki, Inomata, Seishi, Orii, Kazuyuki, Suzuki   +5 more
openaire   +2 more sources

Direct labeling of rat M3-muscarinic receptors by [3H]4DAMP

European Journal of Pharmacology, 1989
The muscarinic receptors of rat submaxillary gland, rat heart and rat cortex were directly labeled using the ligand [3H]4-diphenylacetoxy-N-methyl-piperidine methiodide [( 3H]4DAMP). In the rat submaxillary gland, [3H]4DAMP predominantly bound with high affinity (Kd = 0.2 nM) to a population of binding sites that displayed the pharmacology of the M3 ...
A D, Michel, E, Stefanich, R L, Whiting
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Structure and Transcription of the Human m3 Muscarinic Receptor Gene

American Journal of Respiratory Cell and Molecular Biology, 2002
We have isolated and characterized the human m3 muscarinic receptor gene and its promoter. Using 5' rapid amplification of cDNA ends (RACE), internal polymerase chain reaction (PCR), and homology searching to identify EST clones, we determined that the cDNA encoding the m3 receptor comprises 4,559 bp in 8 exons, which are alternatively spliced to ...
Sean M, Forsythe, Paul C, Kogut, John F, McConville, Yiping, Fu, Joel A, McCauley, Andrew J, Halayko, Hong Wei, Liu, Allen, Kao, Darren J, Fernandes, Shashi, Bellam, Elaine, Fuchs, Satrajit, Sinha, Graeme I, Bell, Blanca, Camoretti-Mercado, Julian, Solway   +14 more
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Interaction of iodinated quinuclidinyl benzilate enantiomers with M3 muscarinic receptors

Life Sciences, 1994
We examined the interaction of 3-quinuclidinyl-4-iodobenzilate enantiomers, (RR)- and (SS)-IQNB, relatively receptor-active and -inactive, respectively, with M3-muscarinic receptors (mAChRs) in rat parotid acinar cells in vitro. This stereospecific antagonist pair has often been used for in vivo studies of mAChRs.
Y, Hiramatsu, W C, Eckelman, B J, Baum
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Prejunctional muscarine receptors in the rabbit ear artery differ from M1, M2 and M3 muscarine receptors

Naunyn-Schmiedeberg's Archives of Pharmacology, 1992
The ability of several selective muscarine receptor antagonists to inhibit the effect of carbachol on prejunctional muscarine receptors on sympathetic nerve endings in the rabbit isolated ear artery was investigated to characterise the receptor subtype involved.
S A, Darroch, L K, Choo, F, Mitchelson
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Long-acting muscarinic M3 receptor antagonists.

Expert opinion on therapeutic patents, 2010
A series of 10 closely related patent applications define Theravance's approach to the development of long-acting M(3) selective antagonists for the treatment of chronic obstructive pulmonary disease. The applications illustrate a modular approach to the design of such agents, comprising a muscarinic pharmacophore attached to a second, less ...
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Activation of M2 muscarinic receptors in guinea-pig ileum opens cationic channels modulated by M3 muscarinic receptors

Life Sciences, 1997
In longitudinal muscle of guinea-pig ileum, activation of muscarinic receptors causes contraction antagonised by M3 receptor subtype antagonists despite a preponderance of M2 receptor subtype binding sites. Experiments on single smooth muscle cells under voltage-clamp described here show that the cationic current evoked by carbachol which normally ...
Bolton, T.B., Zholos, Alexander
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