Pyrimidinylpiperazine
Introduction '''1-(2-Pyrimidinyl)piperazine''' ('''1-PP''', '''1-PmP''') is a chemical compound and piperazine derivative. It is known to act as an antagonist of the α2-adrenergic receptor (Ki = 7.3–40 nM) and, to a much lesser extent, as a partial agonist of the 5-HT1A receptor (Ki = 414 nM; Emax = 54%). It has negligible affinity for the dopamine D2, D3, and D4 receptors (Ki > 10,000 nM) and does not appear to have significant affinity for the α1-adrenergic receptors. Its crystal structure has been determined.
Derivatives A number of pyrimidinylpiperazine derivatives are drugs, including:* Buspirone anxiolytic* Dasatinib anticancer agent* Eptapirone anxiolytic* Gepirone anxiolytic* Ipsapirone anxiolytic* Piribedil antiparkinsonian agent* Revospirone anxiolytic* Tandospirone anxiolytic* Tirilazad neuroprotective agent* Umespirone anxiolytic* Zalospirone anxiolyticThe anxiolytics are also classified as azapirones due to the azaspirodecanedione moiety in their structures. 1-PP is a common metabolite of most or all of the listed agents. Alnespirone, binospirone, and enilospirone, despite being azapirones, are not piperazines and therefore do not metabolize to 1-PP, and while perospirone and tiospirone are piperazines, they are instead benzothiazole-substituted piperazines and do not metabolize to 1-PP either.
See also * Substituted piperazine* Pyridinylpiperazine* Phenylpiperazine* Diphenylmethylpiperazine* Benzylpiperazine
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