Chemistry:Emapunil
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Short description: Chemical compound
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| Formula | C23H23N5O2 |
| Molar mass | 401.470 g·mol−1 |
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Emapunil (AC-5216, XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO.[1][2] This protein has multiple functions, among which is regulation of steroidogenesis,[3][4] particularly the production of neuroactive steroids such as allopregnanolone in the brain.[5][6][7] In both animal and human trials, emapunil produced fast acting anxiolytic and anti-panic effects, without producing sedation or withdrawal symptoms following cessation of use.[8][9] Emapunil is also used in its 11C radiolabelled form to map the distribution of TSPO receptors in the brain.[10][11]
See also
References
- ↑ "Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand". British Journal of Pharmacology 142 (7): 1059–72. August 2004. doi:10.1038/sj.bjp.0705681. PMID 15249420.
- ↑ "Psychiatric Disorders". Drugs of the Future 31 (3): 259. 2006.
- ↑ "Channel-like functions of the 18-kDa translocator protein (TSPO): regulation of apoptosis and steroidogenesis as part of the host-defense response". Current Pharmaceutical Design 13 (23): 2385–405. 2007. doi:10.2174/138161207781368710. PMID 17692008.
- ↑ "Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands". Neuropharmacology 53 (2): 318–29. August 2007. doi:10.1016/j.neuropharm.2007.05.016. PMID 17631921.
- ↑ "Involvement of neurosteroids in the anxiolytic-like effects of AC-5216 in mice". Pharmacology Biochemistry and Behavior 89 (2): 171–8. April 2008. doi:10.1016/j.pbb.2007.12.006. PMID 18201755.
- ↑ "Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis". Journal of Medicinal Chemistry 51 (18): 5798–806. September 2008. doi:10.1021/jm8003224. PMID 18729350.
- ↑ "Translocator Protein Ligands as Promising Therapeutic Tools for Anxiety Disorders". Current Medicinal Chemistry 16 (26): 3359–80. September 2009. doi:10.2174/092986709789057653. PMID 19548867.
- ↑ "Translocator Protein (18 kD) as Target for Anxiolytics Without Benzodiazepine-Like Side Effects". Science 325 (5939): 490–3. June 2009. doi:10.1126/science.1175055. PMID 19541954. Bibcode: 2009Sci...325..490R.
- ↑ "Lack of tolerance to anxiolysis and withdrawal symptoms in mice repeatedly treated with AC-5216, a selective TSPO ligand". Progress in Neuro-psychopharmacology & Biological Psychiatry 33 (6): 1040–5. June 2009. doi:10.1016/j.pnpbp.2009.05.018. PMID 19497344.
- ↑ "11C-AC-5216: a novel PET ligand for peripheral benzodiazepine receptors in the primate brain". Journal of Nuclear Medicine 48 (11): 1853–61. November 2007. doi:10.2967/jnumed.107.043505. PMID 17978354.
- ↑ "Quantitative Analysis of Peripheral Benzodiazepine Receptor in the Human Brain Using PET with 11C-AC-5216". Journal of Nuclear Medicine 50 (7): 1095–101. June 2009. doi:10.2967/jnumed.109.062554. PMID 19525461.
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