Location of a region of the muscarinic acetylcholine receptor involved in selective effector coupling.
Chimaeric muscarinic acetylcholine receptors (mAChR) in which corresponding portions of mAChR I and mAChR II are replaced with each other have been produced in Xenopus oocytes by expression of cDNA constructs encoding them. Functional analysis of the chimaeric mAChRs indicates that a region mostly comprising the putative cytoplasmic portion between the proposed transmembrane segments V and VI is involved in selective coupling of mAChR I and mAChR II with different effector systems. In contrast, the exchange of this region between mAChR I and mAChR II does not significantly affect the antagonist binding properties of the two mAChR subtypes.
Kubo
T
T
Department of Medical Chemistry, Kyoto University Faculty of Medicine, Japan.
Bujo
H
H
Akiba
I
I
Nakai
J
J
Mishina
M
M
Numa
S
S
D000818:Animals; D001483:Base Sequence; D002678:Chimera; D004247:DNA / Q000235:genetics*; D005260:Female; D007700:Kinetics; D008969:Molecular Sequence Data; D009865:Oocytes / Q000378:metabolism; D010890:Pirenzepine / Q000494:pharmacology; D011485:Protein Binding; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D013552:Swine; D014981:Xenopus
D011976:Receptors, Muscarinic; D010890:Pirenzepine; D004247:DNA