Emapunil Explained

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

• SSR-180,575

Notes and References

1. Kita A, Kohayakawa H, Kinoshita T, Ochi Y, Nakamichi K, Kurumiya S, Furukawa K, Oka M . Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand . . 142 . 7 . 1059–72 . August 2004 . 15249420 . 1575165 . 10.1038/sj.bjp.0705681 .
2. Mealy NE, Bayés M, Lupone B, Balcells M . 2006 . Psychiatric Disorders . Drugs of the Future . 31 . 3. 259 .
3. Veenman L, Papadopoulos V, Gavish M . 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 . 17692008 . 10.2174/138161207781368710.
4. Falchi AM, Battetta B, Sanna F, Piludu M, Sogos V, Serra M, Melis M, Putzolu M, Diaz G . Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands . Neuropharmacology . 53 . 2 . 318–29 . August 2007 . 17631921 . 10.1016/j.neuropharm.2007.05.016 . 39793765 .
5. Kita A, Furukawa K . Involvement of neurosteroids in the anxiolytic-like effects of AC-5216 in mice . Pharmacology Biochemistry and Behavior . 89 . 2 . 171–8 . April 2008 . 18201755 . 10.1016/j.pbb.2007.12.006 . 24094283 .
6. Da Settimo F, Simorini F, Taliani S, La Motta C, Marini AM, Salerno S, Bellandi M, Novellino E, Greco G, Cosimelli B, Da Pozzo E, Costa B, Simola N, Morelli M, Martini C . 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 . 18729350 . 10.1021/jm8003224 .
7. Taliani S, Da Settimo F, Da Pozzo E, Chelli B, Martini C . Translocator Protein Ligands as Promising Therapeutic Tools for Anxiety Disorders . Current Medicinal Chemistry . 16. 26. 3359–80. September 2009 . 19548867 . 10.2174/092986709789057653.
8. Rupprecht R, Rammes G, Eser D, Baghai TC, Schüle C, Nothdurfter C, Troxler T, Gentsch C, Kalkman HO, Chaperon F, Uzunov V, McAllister KH, Bertaina-Anglade V, La Rochelle CD, Tuerck D, Floesser A, Kiese B, Schumacher M, Landgraf R, Holsboer F, Kucher K . 26125316 . Translocator Protein (18 kD) as Target for Anxiolytics Without Benzodiazepine-Like Side Effects . Science . 325. 5939. 490–3. June 2009 . 19541954 . 10.1126/science.1175055 . 2009Sci...325..490R .
9. Kita A, Kinoshita T, Kohayakawa H, Furukawa K . 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 . 19497344 . 10.1016/j.pnpbp.2009.05.018 . 8195889 .
10. Zhang MR, Kumata K, Maeda J, Yanamoto K, Hatori A, Okada M, Higuchi M, Obayashi S, Suhara T, Suzuki K . 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 . 17978354 . 10.2967/jnumed.107.043505 . free .
11. Miyoshi M, Ito H, Arakawa R, Takahashi H, Takano H, Higuchi M, Okumura M, Otsuka T, Kodaka F, Sekine M, Sasaki T, Fujie S, Seki C, Maeda J, Nakao R, Zhang MR, Fukumura T, Matsumoto M, Suhara T . 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 . 19525461 . 10.2967/jnumed.109.062554 . free .