Pyrimidinylpiperazine

1-piperazine is a chemical compound and piperazine derivative. It is known to act as an antagonist of the α₂-adrenergic receptor and, to a much lesser extent, as a partial agonist of the 5-HT_1A receptor. It has negligible affinity for the dopamine D₂, D₃, and D₄ receptors 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 – 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.