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 = 7.3–40nM) and, to a much lesser extent, as a partial agonist of the 5-HT1A receptor (Ki = 414nM; Emax = 54%). It has negligible affinity for the dopamine D2, D3, and D4 receptorss (Ki > 10,000nM) and does not appear to have significant affinity for the α1-adrenergic receptorss. 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

References