4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
A series of 4-amino-6-chloro-2-piperazinopyrimidines were synthesized and evaluated for their ability to interact with alpha 1- and alpha 2-adrenoceptors in vitro in binding assays using [3H]WB-4101, [3H]clonidine, and [3H]idazoxan as radioligands. Some compounds were also tested as inhibitors of [3H]spiroperidol binding. Several members of this series showed high and selective affinity for alpha 2-adrenoceptors. The nature of the 4-amino substituent seems to be the most critical factor in determining the potency at these receptors.
D000818:Animals; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism; D003000:Clonidine / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism; D004146:Dioxanes / Q000378:metabolism; D019329:Idazoxan; D010879:Piperazines / Q000378:metabolism*; D011743:Pyrimidines / Q000378:metabolism*; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism; D013329:Structure-Activity Relationship
D004146:Dioxanes; D010879:Piperazines; D011743:Pyrimidines; D011942:Receptors, Adrenergic, alpha; D013134:Spiperone; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane; D003000:Clonidine; D019329:Idazoxan