Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C21H23F3N6O |
| Molecular Weight | 432.4421 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(C=C1CN[C@H]2CCCN[C@H]2C3=CC=CC=C3)N4N=NN=C4C(F)(F)F
InChI
InChIKey=XILNRORTJVDYRH-HKUYNNGSSA-N
InChI=1S/C21H23F3N6O/c1-31-18-10-9-16(30-20(21(22,23)24)27-28-29-30)12-15(18)13-26-17-8-5-11-25-19(17)14-6-3-2-4-7-14/h2-4,6-7,9-10,12,17,19,25-26H,5,8,11,13H2,1H3/t17-,19-/m0/s1
Vofopitant (previously known as GR205171), a tetrazole-derivative, was developed as a neurokinin1 receptor antagonist. Vofopitant was studied in clinical trials phase II for the treatment of primary insomnia and posttraumatic stress disorder. However, these studies were discontinued due to lack of effectiveness. In addition, vofopitant participated in phase I for patients with bipolar disorder. However, this study was terminated because of the slow recruitment; trial unlikely to reach completion.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. | 1996 Aug 27 |
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| Stress-induced increase of cortical dopamine metabolism: attenuation by a tachykinin NK1 receptor antagonist. | 2004 Jan 19 |
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| Ionotropic and metabotropic receptors, protein kinase A, protein kinase C, and Src contribute to C-fiber-induced ERK activation and cAMP response element-binding protein phosphorylation in dorsal horn neurons, leading to central sensitization. | 2004 Sep 22 |
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| Differential effects of dexamethasone, ondansetron and a tachykinin NK1 receptor antagonist (GR205171) on cisplatin-induced changes in behaviour, food intake, pica and gastric function in rats. | 2007 Jan 26 |
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| Increased neurokinin-1 receptor availability in temporal lobe epilepsy: a positron emission tomography study using [(11)C]GR205171. | 2011 Nov |
Patents
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NCI_THESAURUS |
C267
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DB12436
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Vofopitant
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100000087885
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
