Identification of drugs subtype-selective for alpha 2A-, alpha 2B-, and alpha 2C-adrenoceptors in the pig cerebellum and kidney cortex.
The radioligands [3H]MK912 and [3H]RX821002 were used to label alpha2A-, alpha2B-, and alpha2C-adrenoceptors of the pig cerebellum and kidney cortex. By inclusion of the alpha2A-adrenoceptor-selective drug, BRL44408, and using a 'multi-curve' experimental design all the three porcine alpha2-adrenoceptor subtypes could be characterized pharmacologically. The data indicate that the pig alpha2-adrenoceptor subtypes are pharmacologically more related to human alpha2-adrenoceptor subtypes than to the rodent alpha2-adrenoceptors. We suggest a set of drugs that are useful for the delineation of the pig alpha2-adrenoceptor subtypes.
Wikberg-Matsson
A
A
Department of Ophtalmology, Academic Hospital, Uppsala, Sweden.
Wikberg
J E
JE
Uhlén
S
S
D000818:Animals; D001667:Binding, Competitive; D002531:Cerebellum / Q000737:chemistry*; D003984:Dibenzazepines / Q000378:metabolism; D004146:Dioxanes / Q000378:metabolism; D019329:Idazoxan / Q000031:analogs & derivatives; D007093:Imidazoles / Q000378:metabolism; D007672:Kidney Cortex / Q000737:chemistry*; D011807:Quinolizines / Q000378:metabolism; D018341:Receptors, Adrenergic, alpha-2 / Q000145:classification* / Q000378:metabolism; D013552:Swine
D003984:Dibenzazepines; D004146:Dioxanes; D007093:Imidazoles; D011807:Quinolizines; D018341:Receptors, Adrenergic, alpha-2; C054290:L 657743; C072126:BRL 41992; C058525:2-methoxyidazoxan; D019329:Idazoxan