Pyrimidinylpiperazine
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| Template:Longitem | C8H12N4 |
| Molar mass | 164.21 g/mol |
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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)[1] and, to a much lesser extent, as a partial agonist of the 5-HT1A receptor (Ki = 414 nM; Emax = 54%).[2][3] 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.[4]Template:Additional citation needed Its crystal structure has been determined.[5]
Derivatives
A number of pyrimidinylpiperazine derivatives are drugs, including:
- BuspironeTemplate:Snd anxiolytic
- DasatinibTemplate:Snd anticancer agent
- EptapironeTemplate:Snd anxiolytic
- GepironeTemplate:Snd anxiolytic
- IpsapironeTemplate:Snd anxiolytic
- PiribedilTemplate:Snd antiparkinsonian agent
- RevospironeTemplate:Snd anxiolytic
- TandospironeTemplate:Snd anxiolytic
- TirilazadTemplate:Snd neuroprotective agent
- UmespironeTemplate:Snd anxiolytic
- ZalospironeTemplate:Snd 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.[1][6] 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
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