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Muscarinic M3 receptor

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]

Silvetre, J. S., and Prous, J. (2005). Research on adverse drug events Muscarinic m3 receptor binding affinity could predict the risk of antipsycho tics to induce type 2 diabetes. Meth. Find. Exp. Clin. Pharmacol. 27 289-304. [Pg.174]

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]

Pilocarpine directly stimulates the muscarinic (M3) receptors of the ciliary body which causes contraction of the ciliary muscle. This results in widening of the spaces in the trabecular meshwork, which causes an increase in aqueous humor outflow and reduces IOP by 20% to 30%. [Pg.920]

Ecothiophate iodide and denecarium bromide inhibit acetylcholinesterase. Inhibition of this enzyme increases the availability of acetylcholine at the nerve junction, thus increasing the stimulation of the muscarinic (M3) receptors of the ciliary... [Pg.920]

Sawyer, G. W. and Ehlert, F. J. (1999) Muscarinic M3 receptor inactivation reveals a pertussis toxin-sensitive contractile response in the guinea pig colon evidence for M2/M3 receptor interactions../. Pharmacol. Exp. Ther. 289,464-476. [Pg.266]

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]

I. Hellgren, A. Mustafa, M. Riazi, I. Suliman, C. Sylven, A. Adem, Muscarinic M3 receptor subtype gene expression in the human heart. Cell Mol. Life Sci. 57 (2000) 175-180. [Pg.134]

Neural vagal stimulation reieases acetylcholine, which acts on muscarinic M3 receptors, leading to increased cytosoiic Ca2+. [Pg.184]

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]

Khurana S, Yamada M, Wess J, Kennedy RH, Raufman JP (2005) Deoxycholyltaurine-induced vasodilation of rodent aorta is nitric oxide- and muscarinic M3 receptor-dependent. Eur J Pharmacol 517 103-10... [Pg.283]

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

Grillner P, Bonci A, Svensson TH, Bernardi G, Mercuri NB (1999) Presynaptic muscarinic (M3) receptors reduce excitatory transmission in dopamine neurons of the rat mesencephalon. Neuroscience 97 557-565. [Pg.96]

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]

Functional activity at muscarinic receptor subtypes was determined by the use of the muscarinic M2 receptor-mediated negative inotropism in driven guinea pig left atria (1 Hz) and muscarinic M3 receptor-mediated contraction of guinea pig ileum longitudinal muscle. [Pg.330]

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]

Numerous agents are currently undergoing investigation for the management of IBS. Selective blockade of the muscarinic M3 receptors as well as /Ss-adrenoceptor agonists have been shown to alter gut motility without affecting the cardiovascular system. However, two recently tested compounds, zamifenacin and darifenacin have shown limited efficacy to date. ... [Pg.691]

Fig. 1. Schematic representation of the wild-type human Mj and rat Mj receptors, the Mj-trunc and Mj-tail fragments, and the mutants Mj-short and MjfAsndCM Ser) muscarinic receptors. The truncated fragment, M2-trunc, contains the amino-terminal domain, the first five hydrophobic transmembrane regions and the initial portion (56 amino acids) of the third cytoplasmic (i3) loop of the wild-type muscarinic Mj receptor. The M3-tail fragment contains the final portion of the i3 loop (105 amino acids), the last two hydrophobic transmembrane regions and the carboxyl-terminal segment of the wild-type M3 muscarinic receptor. The short construct (Mj-short) represents a receptor in which 196 amino acids of the i3 loop have been deleted the remaining loop is 43 amino acids long. The point mutant MjfAsndOd -> Ser) has the asparagine 404 replaced with serine. The amino acid differences in the transmembrane domains VI and VII of the human muscarinic M2 and the rat muscarinic M3 receptors are presented. Fig. 1. Schematic representation of the wild-type human Mj and rat Mj receptors, the Mj-trunc and Mj-tail fragments, and the mutants Mj-short and MjfAsndCM Ser) muscarinic receptors. The truncated fragment, M2-trunc, contains the amino-terminal domain, the first five hydrophobic transmembrane regions and the initial portion (56 amino acids) of the third cytoplasmic (i3) loop of the wild-type muscarinic Mj receptor. The M3-tail fragment contains the final portion of the i3 loop (105 amino acids), the last two hydrophobic transmembrane regions and the carboxyl-terminal segment of the wild-type M3 muscarinic receptor. The short construct (Mj-short) represents a receptor in which 196 amino acids of the i3 loop have been deleted the remaining loop is 43 amino acids long. The point mutant MjfAsndOd -> Ser) has the asparagine 404 replaced with serine. The amino acid differences in the transmembrane domains VI and VII of the human muscarinic M2 and the rat muscarinic M3 receptors are presented.
Wallis RM. Preclinical and clinical-pharmacology of selective muscarinic M3 receptor antagonists. Life Sci 1995 56 861-868. [Pg.481]


See other pages where Muscarinic M3 receptor is mentioned: [Pg.683]    [Pg.171]    [Pg.377]    [Pg.385]    [Pg.418]    [Pg.115]    [Pg.288]    [Pg.134]    [Pg.1318]    [Pg.1485]    [Pg.283]    [Pg.417]    [Pg.3307]    [Pg.4036]    [Pg.170]    [Pg.171]    [Pg.329]    [Pg.342]    [Pg.256]    [Pg.449]    [Pg.474]    [Pg.476]    [Pg.667]   
See also in sourсe #XX -- [ Pg.385 , Pg.386 ]




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