Sigma receptor ligand N,N'-di-(ortho-tolyl)guanidine inhibits release of acetylcholine in the guinea pig ileum.
The inhibition of stimulated contractions of the guinea pig ileum longitudinal muscle/myenteric plexus preparation by sigma receptor ligands has been previously described. In this study, the stimulated release of [3H]acetylcholine from cholinergic nerve terminals in this same preparation was monitored in the presence and absence of sigma receptor ligands. N,N'-Di-(orthotolyl)guanidine (DTG) and other compounds selective for the sigma receptor inhibited stimulated [3H]acetylcholine release. These results suggest that their inhibition of stimulated contractions in this preparation was mediated by inhibition of acetylcholine release.
Cambell
B G
BG
Vollum Institute, Oregon Health Sciences University, Portland 97201.
Keana
J F
JF
Weber
E
E
D000109:Acetylcholine / Q000378:metabolism*; D000818:Animals; D004558:Electric Stimulation; D005260:Female; D006146:Guanidines / Q000494:pharmacology*; D006168:Guinea Pigs; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000378:metabolism; D011957:Receptors, Opioid / Q000187:drug effects*; D017480:Receptors, sigma; D012701:Serotonin / Q000494:pharmacology
D006146:Guanidines; D011957:Receptors, Opioid; D017480:Receptors, sigma; D012701:Serotonin; C050232:1,3-ditolylguanidine; D000109:Acetylcholine