Inhibitory effect of clonidine on cholinergic transmission.
Equilibrium geometry and electronic structure of three local anesthetic molecules and clonidine were computed. It was shown that clonidine molecule could incorporate into local anesthetic binding centers in potential-operated Na+ channels and in ionic channels coupled to nicotinic cholinergic receptors. The modulatory effect of clonidine on contractile responses of skeletal muscle showed that blockade of Na+ channels and nicotinic cholinergic receptors is a part of its analgesic action.
Katina
I E
IE
V. A. Almazov Cardiology Research Institute, Ministry of Health of the Russian Federation, St. Petersburg. katina@iephb.ru
Nasledov
G A
GA
Khrustaleva
R S
RS
Shchegolev
B F
BF
D000316:Adrenergic alpha-Agonists / Q000737:chemistry / Q000494:pharmacology; D000700:Analgesics / Q000737:chemistry* / Q000494:pharmacology*; D000779:Anesthetics, Local / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D003000:Clonidine / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D009119:Muscle Contraction / Q000187:drug effects; D018482:Muscle, Skeletal / Q000187:drug effects; D018733:Nicotinic Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D009435:Synaptic Transmission / Q000187:drug effects*
D000316:Adrenergic alpha-Agonists; D000700:Analgesics; D000779:Anesthetics, Local; D018733:Nicotinic Antagonists; D003000:Clonidine