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Muscarinic M3 receptor antagonists

DP Mamott, IG Dougall, P Meghani, Y-J Liu, DR Flower. Lead generation using pharmacophore mapping and three-dimensional database searching Application to muscarinic M3 receptor antagonists. J Med Chem 42 3210-3216, 1999. [Pg.366]

Muscarinic M3 receptor Antagonist Acute (gastrointestinal system) Reduced GI motility Darifenacin26... [Pg.112]

Kato M, Komamura K, Kitakaze M. (2006) Tiotropium, a novel muscarinic M3 receptor antagonist, improved symptoms of chronic obstructive pulmonary disease complicated by chronic heart failure. Circ J 70 1658-1660. [Pg.153]

Novel Muscarinic M3 Receptor Antagonist with High Selectivity for M3 over M2 Receptors. J Med Chem 43 5017-5029... [Pg.513]

Bucherer-Bergs products were also the starting points for the preparation of potent and selective muscarinic M3 receptor antagonists (Table 20) [83]. Hydantoins of general structure 228 (Scheme 40) participated in Mitsunobu reactions with alcohols to provide derivatives 229, which were reduced with sodium bis (2-methoxyethoxy)aluminum hydride (Red-Al) to afford imidazolidinones 230. Removal of the benzyl group allowed for further functionalization of the secondary amines to yield compounds 231. [Pg.276]

Wenslow, R.M. solid-state NMR spectroscopic investigation of crystalline and amorphous forms of a selective muscarinic M3 receptor antagonist, in both bulk and pharmaceutical dosage form samples. Drug Dev. Ind. Pharm. 2002, 28 (5), 555-561. [Pg.3310]

Wallis RM. Preclinical and clinical-pharmacology of selective muscarinic M3 receptor antagonists. Life Sci 1995 56 861-868. [Pg.481]

Receptor kinetics, in which slow receptor off-rates have been proposed to lead to enhanced duration of action in both inhaled P2AR agonists and inhaled muscarinic M3 receptor antagonists [12]. [Pg.576]

Muscarinic M3 Receptor. A pharmacophore model was derived from known M3 receptor antagonists, using the program DISCO, and 3D searching was performed by Unity 3D in the Astra Charnwood in-house compound repository and the databases of several commercial suppliers. The 172 compounds that fitted the pharmacophore were screened for their M3-antagonistic potency. Several compounds with micromolar and even submicromolar activities resulted, for example, compound 13 (A50 M3 antagonism 0.2pM pA2 = 6.67 Fig. 16.2) [85],... [Pg.386]

Tsuchiya, Y., Nomoto, T., Ohsawa, H., Kawakami, K., Ohwaki, K., Nishikibe, M. (Banyu Pharmaceutical Co ) Preparation of N-acyl cyclic amine derivatives as selective antagonists of muscarine M3 receptor, W09940070 (1999). [Pg.453]

To test the specificity of PPADS, we compared its blocking activity on P2-purinoceptor-mediated responses with its effects on responses mediated by a -adrenoceptors in rat vas deferens, histamine H]-receptors and muscarinic M3-receptors in guinea-pig ileum, adenosine A j-receptors and muscarinic M2-receptors in guinea-pig atria and adenosine A2-receptors and muscarinic Mj-receptors in rat duodenum. PPADS (100 pM) had no significant effect on either the potency or maximum responses to the respective agonists used in the various receptor preparations. These results demonstrate that the antagonistic effects of PPADS against purine-nucleotides at P2-purinoceptors are specific. [Pg.348]

Dowling, M.R. and Charlton, S.J. (2006) Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor. [Pg.34]

Ml and M3 receptors mediate the excitatory effects and since this postspike hyperpolarisation is blocked by phorbol esters and is therefore presumably dependent on IP3 production, one would expect it to be mediated through M] receptors (see above), especially as these are located postsynaptically. Unfortunately it does not appear to be affected by pirenzapine, the Mi antagonist. By contrast, muscarinic inhibition of the M current is reduced by the Mi antagonist but as it is not affected by phorbol esters is not likely to be linked to IP3 production, an Mi effect. [Pg.128]

The answer is d. (Hardman, pp 142—M3.) ACh will stimulate both muscarinic and nicotinic receptors. Skeletal muscle contraction is mediated through NM receptors, and ganglionic stimulation is an effect of NN receptors All of the other effects listed in the question occur following muscarinic receptor activation and will be blocked by atropine and scopolamine, both of which are muscarinic receptor antagonists. Skeletal muscle contraction will not be affected by these drugs rather, a neuromuscular blocker (e.g., tubocurarine) is required to antagonize this effect of ACh. [Pg.193]

Miyamoto et al. have also demonstrated in the dry skin and itch mouse model (water + acetone ether treated) that the scratching response can be inhibited by the use of atropine, a nonspecific muscarinic acetylcholine receptor (mAChR) antagonist, and 4-diphenyl-acetoxy-N-methyl-piperidine (4-DAMP), an M3 mAChR antagonist.32 They further showed that Mi and M2 mAChR antagonist were not able to inhibit the scratch response. This report suggests the role of acetylcholine, and the M3 specific receptor as a potential player in dry-skin-associated pruritus. In addition, skin biopsies in human subjects with atopic dermatitis were found to have increased levels of acetylcholine compared with normal controls, which suggests that abnormal concentrations of neurotransmitters may also be involved in itch secondary to xeroderma.33... [Pg.130]


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See also in sourсe #XX -- [ Pg.475 ]




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M3 receptor

Muscarin

Muscarine

Muscarine receptors

Muscarines

Muscarinic

Muscarinic M3 antagonists

Muscarinic M3 receptor

Muscarinic antagonists

Muscarinic receptors

Muscarinics

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