The relationship between alpha 2-adrenoceptor selectivity and anticonvulsant effect in a series of clonidine-like drugs.
Clonidine and the 4 clonidine-like drugs: 44-549, lofexidine, guanfacine, and CP-14,304-18, had anticonvulsant activity against pentylenetetrazole-induced convulsions in rats. The magnitude and dose range over which anticonvulsant effects were observed was related to the selectivity of the compounds for alpha 2 and alpha 1 adrenoceptors. Selective alpha 2 adrenoceptor agonists may form a new group of anticonvulsants.
D000818:Animals; D000927:Anticonvulsants; D002540:Cerebral Cortex / Q000187:drug effects / Q000502:physiology / Q000503:physiopathology*; D003000:Clonidine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D005260:Female; D008297:Male; D010433:Pentylenetetrazole; D011224:Prazosin / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011941:Receptors, Adrenergic / Q000502:physiology*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000502:physiology*; D012640:Seizures / Q000503:physiopathology
D000927:Anticonvulsants; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D003000:Clonidine; D010433:Pentylenetetrazole; D011224:Prazosin