Potent and selective α2D
-adrenoceptor agonist (Ki
values are 8.6 pM and 110 nM for rat α2D
receptors respectively and 25, 26 and 100 nM for human α2A
receptors respectively. Exhibits analgesic activity in a mouse model of abdominal irritation. Orally active.
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α2 adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a high-affinity ligand for the α2D adrenergic receptor.
Ross et al.