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M2 muscarinic receptors

Figure 17.7 Possible mechanism by which atypical neuroleptics with antimuscarinic activity produce few EPSs. Normally the inhibitory effects of DA released from nigrostriatal afferents on to striatal neuron D2 receptors is believed to balance the excitatory effect of ACh from intrinsic neurons acting on muscarinic (M2) receptors (a). Typical neuroleptics block the inhibitory effect of DA which leaves unopposed the excitatory effect of ACh (b) leading to the augmented activity of the striatal neurons and EPSs (see Fig. 15.2). An atypical neuroleptic with intrinsic antimuscarinic activity reduces this possibility by counteracting the excitatory effects of released ACh as well as the inhibitory effects of DA (c). Thus the control of striatal neurons remains balanced... Figure 17.7 Possible mechanism by which atypical neuroleptics with antimuscarinic activity produce few EPSs. Normally the inhibitory effects of DA released from nigrostriatal afferents on to striatal neuron D2 receptors is believed to balance the excitatory effect of ACh from intrinsic neurons acting on muscarinic (M2) receptors (a). Typical neuroleptics block the inhibitory effect of DA which leaves unopposed the excitatory effect of ACh (b) leading to the augmented activity of the striatal neurons and EPSs (see Fig. 15.2). An atypical neuroleptic with intrinsic antimuscarinic activity reduces this possibility by counteracting the excitatory effects of released ACh as well as the inhibitory effects of DA (c). Thus the control of striatal neurons remains balanced...
Datta, S., Quattrochi, J. J. Hobson, J. A. (1993). Effect of specific muscarinic M2 receptor antagonist on carbachol induced long-term REM sleep. Sleep 16, 8-14. [Pg.49]

Muscarinic M2 receptor CHRM2 Agonism Vagal effects (key role in the control of heart rate and smooth muscle activity) Bradycardia. Antagonism May induce cardiac side effects (palpitations, dysrhythmia) or peripheral edema, bronchoconstriction can result from presynaptic M2 receptor antagonism if postsynaptic M3 receptors are not also blocked. [Pg.282]

Biinemann, M., Brandts, B., and Pott, L. (1996). Downregulation of muscarinic M2 receptors linked to K+ current in cultured guinea-pig atrial myocytes. J. Physiol. 494, 351-362. [Pg.186]

Tucek, S., P. Michal, and V. Vlachova. 2001. Dual effects of muscarinic M2 receptors on the synthesis of cyclic AMP in CHO cells background and model. Life Sci. 68 2501-2510. [Pg.191]

Schroter, A., C. Trankle, and K. Mohr. 2000. Modes of allosteric interactions with free and [3H] N-methylscopolamine-occupied muscarinic M2 receptors as deduced from buffer-dependent potency shifts. Naun. Schmied. Arch. Pharmacol. 362, 512-519. [Pg.23]

Bemardini N, Roza C, Sauer SK, Gomeza J, Wess J, Reeh PW (2002) Muscarinic M2 receptors on peripheral nerve endings a molecular target of antinociception. J Neurosci 22 RC229 Bemardini N, Sauer SK, Haberberger R, Fischer MJM, Reeh PW (2001) Excitatory nicotinic and desensitizing muscarinic (M2) effects on C-nociceptors in isolated rat skin. J Neurosci 21 3295-3302... [Pg.487]

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]

Furthermore, it turned out that tripitramine has not only an outstanding affinity and selectivity for muscarinic M2 receptors but also a superior specificity compared with methoctramine. In addition to muscarinic receptors, tripitramine inhibited only frog rectus abdominis muscular (pICso value of 6.14) and rat duodenum neuronal (pICso value of 4.87) nicotinic receptors among receptor systems investigated, namely ap, a.2-, and f3i-adrenoceptors, Hp and H2-histamine receptors, and muscular and neuronal nicotinic receptors [55]. [Pg.333]

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]

Fig. 89. Comparison between the distribution of m2 muscarine receptor mRNA (A) and [ H]oxotremorine-M binding to muscarine M2 receptor sites (B) in approximately equivalent coronal sections of rat brain at the level of the caudal cerebellum. Note that m2 mRNAs in the ventral uvula (IX) and the nodulus are localized in the granular layer, whereas M2 receptor binding sites are in the molecular layer (m). 12, hypoglossal nucleus. Scale bar = 3 mm. Vilaro et al. (1992). Fig. 89. Comparison between the distribution of m2 muscarine receptor mRNA (A) and [ H]oxotremorine-M binding to muscarine M2 receptor sites (B) in approximately equivalent coronal sections of rat brain at the level of the caudal cerebellum. Note that m2 mRNAs in the ventral uvula (IX) and the nodulus are localized in the granular layer, whereas M2 receptor binding sites are in the molecular layer (m). 12, hypoglossal nucleus. Scale bar = 3 mm. Vilaro et al. (1992).
Summarizing it appears that the cellular and regional distribution of muscarine receptors in the cerebellum is different between different species. Golgi cells and subpopulations of mossy fibers seem to express muscarine receptors most constantly. An interesting aspect about the presence of muscarine receptors in parallel fibers in rat and rabbit, is that the lobular distribution of m2-containing parallel fibers, is the same as that of ChAT-positive mossy fiber rosettes (see above). This raises the possibility that muscarine m2 receptor are specifically expressed by those granule cells that are innervated by cholinergic mossy fibers. If this proves to be true, this would imply that there... [Pg.125]

It should be noted that the distribution of most markers, as identified in rodent species, may be different in other species or, as is the case for the muscarine m2 receptors, may be expressed in specific species only (Neustadt et al, 1988) (see Section... [Pg.189]

Aubert I, Cecyre D, Gauthier S, Quirion R (1992) Characterization and auto-radiographic distribution of [ H]AF-DX 384 binding to putative muscarinic M2 receptors in the rat brain. Eur. J. Pharmacol, 217, 173-184. [Pg.313]

Vilaro MT, Wiederhold K-H, Palacios JM, Mengod G (1992) Muscarinic M2 receptor mRNA expression and receptor binding in cholinergic and non-cholinergic cells in the rat brain a correlative study using in situ hybridization histochemistry and receptor autoradiography. Neuroscience, 47, 367 -393. [Pg.365]

Heitz, F., Holzwarth, J.A., Gies, J.-P., Pmss, R.M., Trumpp-Kallmeyer, S., Hibert, M. and Guenet, C. (1999) Site directed mutagenesis of the putative human muscarinic M2 receptor binding site. Eur. J. Pharmacol 380 183-195. [Pg.64]

Muscarinic M2 receptor CV Tachycardia, vagal changes, blood pressure changes... [Pg.73]

Management Muscarinic M2 receptors in the vagus are involved in the cardiotoxicity of grayanotoxin [112", 113" ], and bradycardia and heart block in these cases respond to atropine, as in toxicity with vera-trum alkaloids. However, temporary pacing may sometimes be required [114 ]. [Pg.998]

Michal P, Rudajev V, El-Fakahany EE, Dolezal V. Membrane cholesterol content influences binding properties of muscarinic M2 receptors and differentially impacts activation of second messenger pathways. EurJ Pharmacol. 2009 606(l-3) 50-60. [Pg.178]


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See also in sourсe #XX -- [ Pg.59 , Pg.61 ]




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M2 receptor

Ml and M2-muscarinic receptors

Muscarin

Muscarine

Muscarine receptors

Muscarines

Muscarinic

Muscarinic receptors

Muscarinics

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