scholarly journals Functional role in ligand binding and receptor activation of an asparagine residue present in the sixth transmembrane domain of all muscarinic acetylcholine receptors.

1994 ◽  
Vol 269 (29) ◽  
pp. 18870-18876
Author(s):  
K. Blüml ◽  
E. Mutschler ◽  
J. Wess
Keyword(s):  
Ligand Binding ◽  
Acetylcholine Receptors ◽  
Functional Role ◽  
Transmembrane Domain ◽  
Receptor Activation ◽  
Muscarinic Acetylcholine Receptors ◽  
Muscarinic Acetylcholine ◽  
Asparagine Residue

scholarly journals BRET- and fluorescence anisotropy-based assays for real-time monitoring of ligand binding to M2 muscarinic acetylcholine receptors

2021 ◽  
Vol 1868 (3) ◽  
pp. 118930
Author(s):  
Lukas Grätz ◽  
Tõnis Laasfeld ◽  
Anni Allikalt ◽  
Corinna G. Gruber ◽  
Andrea Pegoli ◽  
...  
Keyword(s):  
Ligand Binding ◽  
Real Time ◽  
Fluorescence Anisotropy ◽  
Acetylcholine Receptors ◽  
Muscarinic Acetylcholine Receptors ◽  
Real Time Monitoring ◽  
Muscarinic Acetylcholine

scholarly journals Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors.

1987 ◽  
Vol 6 (13) ◽  
pp. 3923-3929 ◽  
Author(s):  
E. G. Peralta ◽  
A. Ashkenazi ◽  
J. W. Winslow ◽  
D. H. Smith ◽  
J. Ramachandran ◽  
...  
Keyword(s):  
Ligand Binding ◽  
Acetylcholine Receptors ◽  
Muscarinic Acetylcholine Receptors ◽  
Binding Properties ◽  
Specific Expression ◽  
Tissue Specific ◽  
Tissue Specific Expression ◽  
Muscarinic Acetylcholine ◽  
Primary Structures

Propofol-induced Depression of Cultured Rat Ventricular Myocytes Is Related to the M2-acetylcholine Receptor–NO–cGMP Signaling Pathway 

1999 ◽  
Vol 91 (6) ◽  
pp. 1712-1712 ◽  
Author(s):  
Shuji Yamamoto ◽  
Shin Kawana ◽  
Atsushi Miyamoto ◽  
Hideyo Ohshika ◽  
Akiyoshi Namiki
Keyword(s):  
Acetylcholine Receptor ◽  
Acetylcholine Receptors ◽  
Ventricular Myocytes ◽  
Receptor Activation ◽  
Muscarinic Acetylcholine Receptors ◽  
No Production ◽  
Dependent Manner ◽  
Rat Ventricular Myocytes ◽  
Muscarinic Acetylcholine ◽  
Nitrite Production

Background It is well-known that propofol sometimes causes bradycardia or asystole during anesthesia; however, the direct effect of propofol on the myocardium remains unclear. Previous reports showed the contribution of muscarinic acetylcholine receptors to propofol-induced bradycardia. Conversely, it was suggested recently that nitric oxide (NO) plays an important role in mediating the effect of vagal stimulation in the autonomic regulation of the heart. Therefore, the authors investigated the effects of propofol on spontaneous contraction and NO production in cultured rat ventricular myocytes. Methods The authors measured chronotropic responses of cultured rat ventricular myocytes induced by propofol stimulation with a sensor, a fiber-optic displacement measurement instrument. The authors also quantitatively analyzed NO metabolite production in cultured myocytes by measuring the levels of nitrite and nitrate in a high-performance liquid chromatography reaction system. The influence of propofol on muscarinic acetylcholine receptors of myocyte membranes was also measured with a competitive binding assay using [3H]quinuclidinyl benzilate ([3H]QNB). Results Propofol caused negative chronotropy in a dose-dependent manner. Propofol (IC50) also caused the enhancement of nitrite production in cultured myocytes. Eighty percent of the enhancement of nitrite production induced by propofol (IC50) stimulation was abolished by pretreatment with atropine, methoctramine, or N(G)-monomethyl-L-arginine acetate (L-NMMA). The negative chronotropy induced by propofol (IC50) stimulation was reduced to 40-50% by pretreatment with atropine, methoctramine, L-NMMA, or 1H[1,2,4]oxadiazolo[4,3-alpha]quanoxalin-1-one, a selective inhibitor of guanylyl cyclase. Propofol displaced [3H]QNB binding to the cell membrane of myocytes in a concentration-dependent manner. Conclusion These results suggest that the negative chronotropy induced by propofol is mediated in part by M2-acetylcholine receptor activation, which involves the enhancement of NO production in cultured rat ventricular myocytes.

Sign in / Sign up

Export Citation Format

Share Document