Results 91 to 100 of about 1,546 (109)

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
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Structure and Transcription of the Human m3 Muscarinic Receptor Gene

American Journal of Respiratory Cell and Molecular Biology, 2002
Abstract 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 ...
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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Distribution of muscarinic receptor subtype M3 in melanomas and their metastases

Journal of Cutaneous Pathology, 2008
Background:  Muscarinic acetylcholine receptors (mR) are involved in the regulation of cancer cell motility and cancer progression. mR have been shown in melanoma cell lines and cryostat sections of melanomas. To substantiate the experimental data, here the correlation of mR‐expression with invasive growth was studied on the cellular level by ...
Matthias, Oppitz, Christian, Busch, Claus, Garbe, Ulrich, Drews   +3 more
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Potassium, M3 muscarinic receptors, and dopamine release

Neuroscience Research Communications, 2001
AbstractThe factors determining dopamine (DA) release induced by muscarinic receptor stimulation were investigated. Carbachol facilitated DA release elicited by electrical stimulation (1Hz, 2 min). In addition, carbachol per se induced DA release (direct action); an effect dependent of potassium levels. Increasing potassium from 4.8 to 12.5 mM produced
I.S. Hoffmann, B.H. Guevara, L.X. Cubeddu   +2 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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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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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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Mice lacking the M3 muscarinic acetylcholine receptor are hypophagic and lean

Nature, 2001
Members of the muscarinic acetylcholine receptor family (M1-M5) have central roles in the regulation of many fundamental physiological functions. Identifying the specific receptor subtype(s) that mediate the diverse muscarinic actions of acetylcholine is of considerable therapeutic interest, but has proved difficult primarily because of a lack of ...
M, Yamada, T, Miyakawa, A, Duttaroy, A, Yamanaka, T, Moriguchi, R, Makita, M, Ogawa, C J, Chou, B, Xia, J N, Crawley, C C, Felder, C X, Deng, J, Wess   +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.
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The endegenous muscarinic acetylcholine receptor in Xenopus oocytes is of the M3 subtype

European Journal of Pharmacology, 1988
The muscarinic acetylcholine receptor of the Xenopus oocyte was characterized electrophysiologically. Iontophoretic responses to acetylcholine were inhibited by the muscarinic antagonists 4-DAMP, pirenzepine and AF-DX 116 at respective IC50 values of 7 nM, 15 microM and 2 microM.
L A, Van Wezenbeek, J A, Tonnaer, G S, Ruigt   +2 more
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