Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C8H12N4 |
| Molecular Weight | 164.2077 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C1CN(CCN1)C2=NC=CC=N2
InChI
InChIKey=MRBFGEHILMYPTF-UHFFFAOYSA-N
InChI=1S/C8H12N4/c1-2-10-8(11-3-1)12-6-4-9-5-7-12/h1-3,9H,4-7H2
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| A comparative multidose pharmacokinetic study of buspirone extended-release tablets with a reference immediate-release product. | 2001 Aug |
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| Pharmacokinetics and tolerability of buspirone during oral administration to children and adolescents with anxiety disorder and normal healthy adults. | 2001 Dec |
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| Pharmacokinetics of buspirone extended-release tablets: a single-dose study. | 2001 Jul |
|
| Conformational analysis and pharmacophore design for selected 1-(2-pyrimidinyl)piperazine derivatives with sedative-hypnotic activity. | 2001 Mar-Apr |
|
| The biphasic immunoregulation of pyrimidylpiperazine (Y-40138) is IL-10 sensitive and requires NF-kappa B targeting in the alveolar epithelium. | 2001 May |
|
| Oxygen-sensing mechanisms and the regulation of redox-responsive transcription factors in development and pathophysiology. | 2002 |
|
| Factors explaining variance in perceived pain in women with fibromyalgia. | 2002 Apr 25 |
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| Pharmacokinetic-pharmacodynamic modeling of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in rats. | 2002 Dec |
|
| Pharmacological properties and SAR of new 1,4-disubstituted piperazine derivatives with hypnotic-sedative activity. | 2002 May |
|
| Effects of the serotonergic anxiolytic buspirone on plasma glucose and glucose-induced hyperglycemia in mice. | 2003 Dec |
|
| Effect of the novel anxiolytic drug deramciclane on the pharmacokinetics and pharmacodynamics of the CYP3A4 probe drug buspirone. | 2003 Dec |
|
| Science review: redox and oxygen-sensitive transcription factors in the regulation of oxidant-mediated lung injury: role for hypoxia-inducible factor-1alpha. | 2003 Feb |
|
| In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity. | 2003 Jan 10 |
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| Human cytochromes mediating gepirone biotransformation at low substrate concentrations. | 2003 Mar |
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| Pharmacokinetic evaluation of gepirone immediate-release capsules and gepirone extended-release tablets in healthy volunteers. | 2003 Sep |
|
| 1-(2-pyrimidinyl)-piperazine, a buspirone metabolite, modulates bladder function in the anesthetized rat. | 2004 |
|
| The photocatalytic process as a tool to identify metabolitic products formed from dopant substances: the case of buspirone. | 2004 Apr 1 |
|
| Combination benefit of a pyrimidylpiperazine derivative (Y-40138) and methotrexate in arthritic rats. | 2004 Aug 30 |
|
| Inhibitory effects of the 5-HT(1A) receptor agonist buspirone on stress-induced hyperglycemia in mice: involvement of insulin and a buspirone metabolite, 1-(2-pyrimidinyl)piperazine (1-PP). | 2005 Apr |
|
| Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. | 2005 Apr |
|
| Cyp2D6 catalyzes 5-hydroxylation of 1-(2-pyrimidinyl)-piperazine, an active metabolite of several psychoactive drugs, in human liver microsomes. | 2005 Feb |
|
| Oral buspirone causes a shift in the dose-response curve between the elevated-plus maze and Vogel conflict tests in Long-Evans rats: relation of brain levels of buspirone and 1-PP to anxiolytic action. | 2005 May |
|
| Pharmacokinetics of buspirone in autistic children. | 2006 May |
|
| 6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats. | 2007 Aug |
|
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. | 2007 Jul 26 |
|
| Pharmacokinetics of 6-hydroxybuspirone and its enantiomers administered individually or following buspirone administration in humans. | 2007 Oct |
|
| A novel p38 alpha MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer's disease mouse model. | 2007 Sep 4 |
|
| TRPV1: a target for next generation analgesics. | 2008 Jun |
|
| Mass spectrometry analysis of phosphopeptides after peptide carboxy group derivatization. | 2008 Nov 1 |
|
| Pharmacokinetic interaction between tandospirone and fluvoxamine in the rat contextual conditioned fear stress model and its functional consequence: Involvement of cytochrome P450 3A4. | 2008 Oct |
|
| Group 11 metal chemistry of a tetradentate ligand, phenylene-1,4-diaminotetra(phosphonite), p-C6H4[N{P(OC6H4OMe-o)2}2]2. | 2009 Apr 20 |
|
| Carboxy group derivatization for enhanced electron-transfer dissociation mass spectrometric analysis of phosphopeptides. | 2009 Aug |
|
| Cyndi: a multi-objective evolution algorithm based method for bioactive molecular conformational generation. | 2009 Mar 31 |
|
| Two-injection workflow for a liquid chromatography/LTQ-Orbitrap system to complete in vivo biotransformation characterization: demonstration with buspirone metabolite identification. | 2009 Sep |
|
| A new strategy for antidepressant prescription. | 2010 |
|
| Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators. | 2010 Feb 1 |
|
| Synthesis and biological activity of some novel trifluoromethyl-substituted 1,2,4-triazole and bis(1,2,4-triazole) Mannich bases containing piperazine rings. | 2010 May 12 |
|
| Moving towards supraspinal TRPV1 receptors for chronic pain relief. | 2010 Oct 11 |
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| Code System | Code | Type | Description | ||
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244-135-5
Created by
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1078573
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Pyrimidinylpiperazine
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88747
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H3B5B38F56
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20980-22-7
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DTXSID00864967
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PARENT (METABOLITE ACTIVE)
SUBSTANCE RECORD
