The alpha 2-adrenoceptor antagonist SK&F 104078 has high affinity for 5-HT1A and 5-HT2 receptors.
The affinity of SK&F 104078, a putative selective postjunctional alpha 2-adrenoceptor antagonist, was determined at 5-HT1A and 5-HT2 receptors in rat brain. SK&F 104078 had moderate affinity towards alpha 2-adrenoceptors (pKi 6.7) but displayed higher affinity at 5-HT1A (pKi 8.1) and 5-HT2 (pKi 7.6) receptors. If SK&F 104078 is used in functional studies to define heterogeneity within of alpha 2-adrenoceptors, care must be taken to define the role of 5-HT1A and 5-HT2 receptors in the response being measured.
Kilpatrick
A T
AT
Department of Pharmacology, Syntex Research Centre, Riccarton, Edinburgh, U.K.
Brown
C M
CM
MacKinnon
A C
AC
Spedding
M
M
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000317:Adrenergic alpha-Antagonists / Q000378:metabolism*; D000818:Animals; D001552:Benzazepines / Q000378:metabolism*; D001667:Binding, Competitive / Q000187:drug effects; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D007650:Ketanserin / Q000037:antagonists & inhibitors; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism*; D013764:Tetrahydronaphthalenes / Q000037:antagonists & inhibitors
D000317:Adrenergic alpha-Antagonists; D001552:Benzazepines; D011942:Receptors, Adrenergic, alpha; D011985:Receptors, Serotonin; D013764:Tetrahydronaphthalenes; C054935:SK&F 104078; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D007650:Ketanserin