[Adrenergic receptor and alpha 2 agonist--2: Function analysis of adrenoceptor subtype by knockout mice and knockdown rats].
Alpha 2 adrenergic agonists will soon be used in the anesthetic management for their sedative/hypnotic, anesthetic-sparing, analgesic and sympatholytic properties. But the clinically available alpha 2 agonists have unwanted side-effects such as acute hypertension and bradycardia following a bolus injection because these agonists do not discriminate between the 3 alpha 2 adrenoceptor subtypes. Molecular biological methods can identify mediating receptor subtype for each response. Knockout mice study reveals that the alpha 2 B adrenoceptor subtype mediates the hypertensive response to alpha 2 agonists. Knockdown study using the antisense technology demonstrates that the alpha 2 A adrenoceptor subtype mediates the hypnotic and analgesic effects of alpha 2 agonists. The next generation of alpha 2 agonists should be alpha 2 A selective to maximize anesthetic and analgesic effects while minimizing hypertensive response.
Mizobe
T
T
Department of Anesthesiology, Kyoto Prefectural, University of Medicine.
D000316:Adrenergic alpha-Agonists / Q000009:adverse effects / Q000494:pharmacology; D000818:Animals; D001919:Bradycardia / Q000139:chemically induced; D016373:DNA, Antisense / Q000494:pharmacology; D006973:Hypertension / Q000139:chemically induced; D007093:Imidazoles / Q000009:adverse effects / Q000494:pharmacology; D020926:Medetomidine; D051379:Mice; D018345:Mice, Knockout; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000145:classification / Q000187:drug effects
D000316:Adrenergic alpha-Agonists; D016373:DNA, Antisense; D007093:Imidazoles; D011942:Receptors, Adrenergic, alpha; D020926:Medetomidine