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Pyrimidinylpiperazine

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 α<sub>2</sub>-adrenergic receptor (K<sub>i</sub> = 7.3–40&nbsp;nM) and, to a much lesser extent, as a partial agonist of the 5-HT<sub>1A</sub> receptor (K<sub>i</sub> = 414&nbsp;nM; E<sub>max</sub> = 54%). It has negligible affinity for the dopamine D<sub>2</sub>, D<sub>3</sub>, and D<sub>4</sub> receptors (K<sub>i</sub> > 10,000&nbsp;nM) and does not appear to have significant affinity for the α<sub>1</sub>-adrenergic receptors. Its crystal structure has been determined.

Derivatives

A number of pyrimidinylpiperazine derivatives are drugs, including:

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

References