TP-003
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Chemical compound
Pharmaceutical compound
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| Formula | C23H16F3N3O |
| Molar mass | 407.396 g·mol−1 |
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TP-003 is an anxiolytic drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.
TP-003 is a positive allosteric modulator at the benzodiazepine binding site of GABAA receptors.[1] It possesses relative selectivity for benzodiazepine sites on α3-containing GABAA receptors, which are thought to contribute to the anxiolytic effects of benzodiazepines (in tandem with those containing α2 subunits).[2] It has modest anticonvulsant activity although less than that of diazepam.[3]
References
- ↑ Neumann E, Ralvenius WT, Acuña MA, Rudolph U, Zeilhofer HU (2018). "TP003 is a non-selective benzodiazepine site agonist that induces anxiolysis via α2GABAA receptors". Neuropharmacology. 143: 71–78. doi:10.1016/j.neuropharm.2018.09.026. PMID 30240781. S2CID 52313196.
- ↑ Rudolph U, Möhler H (2013-10-23). "GABAA receptor subtypes: Therapeutic potential in Down syndrome, affective disorders, schizophrenia, and autism". Annual Review of Pharmacology and Toxicology. 54: 483–507. doi:10.1146/annurev-pharmtox-011613-135947. PMC 3997216. PMID 24160694.
- ↑ Fradley RL, Guscott MR, Bull S, Hallett DJ, Goodacre SC, Wafford KA, et al. (Jun 2007). "Differential contribution of GABA(A) receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands". Journal of Psychopharmacology. 21 (4): 384–91. doi:10.1177/0269881106067255. PMID 17092983. S2CID 34355306.
