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 (indicated for Major depressive disorder) Ipsapirone anxiolytic Piribedil antiparkinsonian agent Revospirone anxiolytic Tandospirone anxiolytic Tirilazad neuroprotective agent Umespirone anxiolytic Zalospirone anxiolytic
The 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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