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Emapunil

Clinical data
ATC code	none
Identifiers
IUPAC name N-benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenylpurin-9-yl)acetamide
CAS Number	226954-04-7
PubChem CID	6433109
UNII	OG837L732J
CompTox Dashboard (EPA)	DTXSID40177220
Chemical and physical data
Formula	C23H23N5O2
Molar mass	401.461 g/mol g·mol
(verify)

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. This protein has multiple functions, among which is regulation of steroidogenesis, particularly the production of neuroactive steroids such as allopregnanolone in the brain. 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. Emapunil is also used in its C radiolabelled form to map the distribution of TSPO receptors in the brain.

References

1. Kita A, Kohayakawa H, Kinoshita T, Ochi Y, Nakamichi K, Kurumiya S, Furukawa K, Oka M (2004). "Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand". British Journal of Pharmacology. 142 (7): 1059–72. doi:10.1038/sj.bjp.0705681. PMC 1575165. PMID 15249420. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
2. Mealy NE, Bayés M, Lupone B, Balcells M (2006). "Psychiatric Disorders". Drugs of the Future. 31 (3): 259.{{cite journal}}: CS1 maint: multiple names: authors list (link)
3. Veenman L, Papadopoulos V, Gavish M (2007). "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. doi:10.2174/138161207781368710. PMID 17692008.{{cite journal}}: CS1 maint: multiple names: authors list (link)
4. Falchi AM, Battetta B, Sanna F, Piludu M, Sogos V, Serra M, Melis M, Putzolu M, Diaz G (2007). "Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands". Neuropharmacology. 53 (2): 318–29. doi:10.1016/j.neuropharm.2007.05.016. PMID 17631921. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
5. Kita A, Furukawa K (2008). "Involvement of neurosteroids in the anxiolytic-like effects of AC-5216 in mice". Pharmacology, Biochemistry, and Behavior. 89 (2): 171–8. doi:10.1016/j.pbb.2007.12.006. PMID 18201755. {{cite journal}}: Unknown parameter |month= ignored (help)
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 (2008). "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. doi:10.1021/jm8003224. PMID 18729350. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
7. Taliani S, Da Settimo F, Da Pozzo E, Chelli B, Martini C (2009). "Translocator Protein Ligands as Promising Therapeutic Tools for Anxiety Disorders". Current Medicinal Chemistry. 16 (26): 3359–80. doi:10.2174/092986709789057653. PMID 19548867. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
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 (2009). "Translocator Protein (18 kD) as Target for Anxiolytics Without Benzodiazepine-Like Side Effects". Science. 325 (5939): 490–3. doi:10.1126/science.1175055. PMID 19541954. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
9. Kita A, Kinoshita T, Kohayakawa H, Furukawa K (2009). "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. doi:10.1016/j.pnpbp.2009.05.018. PMID 19497344. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
10. Zhang MR, Kumata K, Maeda J, Yanamoto K, Hatori A, Okada M, Higuchi M, Obayashi S, Suhara T, Suzuki K (2007). "11C-AC-5216: a novel PET ligand for peripheral benzodiazepine receptors in the primate brain". Journal of Nuclear Medicine. 48 (11): 1853–61. doi:10.2967/jnumed.107.043505. PMID 17978354. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
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 (2009). "Quantitative Analysis of Peripheral Benzodiazepine Receptor in the Human Brain Using PET with 11C-AC-5216". Journal of Nuclear Medicine. 50 (7): 1095–101. doi:10.2967/jnumed.109.062554. PMID 19525461. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

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