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Alvameline

CAS No. : 120241-31-8

MCE 站：Alvameline

产品活性：Alvameline (Lu25-109)是M1的部分激动剂，也是M2/M3拮抗剂。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mAChR

In Vitro: Alvameline is metabolized by human liver microsomes to Lu 31-126 mainly by CYP2D6; to Lu 29-297 and Lu 25-077 mainly by CYP1A2, CYP2A6, CYP2C19, and CYP3A4; and to Lu 32-181 by CYP1A2 and possibly by CYP2C19. One metabolite, Lu 32-181, could be reduced back to alvameline, a reaction not inhibited by the applied cytochrome P-450 inhibitors.

In Vivo: Alvameline competitively and effectively antagonizes carbachol-induced contractions and contractions induced by electrical field stimulation in human detrusor muscle. Alvameline produces a concentration-dependent rightward shift of the concentration-response curves for carbachol in both human and pig detrusor, the pK_b values being 6.2 and 5.8. Contractions induced by electrical field stimulation in human detrusor are almost completely inhibited by 100 μM alvameline. In contrast, electrical field stimulation-induced contractions in pig detrusor are less sensitive to alvameline, resulting in a final inhibition of 32% with the highest concentration used (100 μM). Alvameline has been shown to improve cognitivefunction following traumatic brain injury in rats. Alvameline treated rats causes a 13% and 5% decrease in the medial septal nucleus, a 48 and 23% decrease in the vertical limb nucleus of the diagonal band, and a 51 and 28% decrease in the nucleus basalis magnocellularis, respectively.

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