MULTISCREEN™ MEMBRANE PREPARATION
HUMAN RECOMBINANT M5 RECEPTOR
Expression vector containing full-length human CHRM5 cDNA (GenBank accession Number NM_012125) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Background: The muscarinic M5 receptor is a 532-amino acid 7-transmembrane protein. Acetylcholine, a potent dilator of most vascular beds, virtually lost the ability to dilate cerebral arteries and arterioles in M5 -/- mice, suggesting that endothelial M5 receptors mediate this activity in wild-type mice. M5 receptors located on dopaminergic nerve terminals play a role in facilitating muscarinic agonist-induced dopamine release in the striatum. Both somatic and affective components of naloxone-induced morphine withdrawal symptoms were significantly attenuated in M5 -/- mice. M5 receptor activity modulates both morphine reward and withdrawal processes, suggesting that M5 receptors may represent a novel target for the treatment of opiate addiction.
Figure 1. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells. Thin line: parental cells; thick line: receptor-expressing cells.
Basile et al. (2002) Deletion of the M5 muscarinic acetylcholine receptor attenuates morphine reinforcement and withdrawal but not morphine analgesia. Proc Natl Acad Sci USA 99:11452-11457.
Yamada et al. (2003) Novel insights into M5 muscarinic acetylcholine receptor function by the use of gene targeting technology. Life Sci 74:345-353.