AC-5216
AC-5216 Basic information
- Product Name:
- AC-5216
- Synonyms:
-
- EMapunil
- XBD-173
- N-Benzyl-N-ethyl-2-(7-Methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetaMide
- 9H-Purine-9-acetaMide,N-ethyl-7,8-dihydro-7-Methyl-8-oxo-2-phenyl-N-(phenylMethyl)-
- AC 5216 (Emapunil)
- N-Ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-N-(phenylmethyl)-9H-purine-9-acetamide
- Emapunil(AC-5216)
- AC-5216
- CAS:
- 226954-04-7
- MF:
- C23H23N5O2
- MW:
- 401.46
- Product Categories:
-
- Inhibitors
- Mol File:
- 226954-04-7.mol
AC-5216 Chemical Properties
- storage temp.
- 2-8°C
- solubility
- DMF: 30 mg/mL; DMF:PBS (pH 7.2) (1:20): 0.05 mg/mL; DMSO: 5 mg/mL
- form
- powder
- color
- white to beige
- InChI
- 1S/C23H23N5O2/c1-3-27(15-17-10-6-4-7-11-17)20(29)16-28-22-19(26(2)23(28)30)14-24-21(25-22)18-12-8-5-9-13-18/h4-14H,3,15-16H2,1-2H3
- InChIKey
- NBMBIEOUVBHEBM-UHFFFAOYSA-N
- SMILES
- CN(C1=CN=C(C2=CC=CC=C2)N=C1N3CC(N(CC)CC4=CC=CC=C4)=O)C3=O
AC-5216 Usage And Synthesis
Uses
Emapunil possesses anxiolytic and antidepressant-like effects and a ligand for translocator protein (TSPO), which plays an important role in the depression treatment.
Biochem/physiol Actions
XBD173 (emapunil, AC-5216) is a potent and selective translocator protein 18 kDa (TSPO) ligand with a Ki value of 0.297 nM. XBD173 acts at the TSPO translocator protein, formerly called the peripheral benzodiazepine receptor, which is involved in production of neuroactive steroids such as allopregnanolone in the brain. TSPO carries cholesterol from the outer to the inner mitochondrial membrane, which is the rate-limiting step of steroidogenesis. XBD173 enhances GABA-mediated neurotransmission via induction of neurosteroidogenesis and exhibits anti-anxiety and antidepressant-like effects.
in vivo
Emapunil (AC-5216, 0.1-3, 0.003-0.01 and 0.01-0.3 mg/kg, p.o.) produces anti-anxiety effects in the Vogel-type conflict test in rats, and in the light/dark box and social interaction tests in mice[1].
Emapunil (AC-5216, 3-30 mg/kg, p.o.) reduces the immobility time, and this effect was blocked by PK11195[1].
Emapunil (AC-5216, 1-100 mg/kg, p.o.) produces no distinct change in the rat electroencephalogram[1].
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) causes significant suppression of the enhanced anxiety and contextual fear induced in post-TDS rats[3].
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) alleviates the enhanced anxiety and fear response in a time-dependent sensitization (TDS) procedure, a rat PTSD animal model[3].
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) reverses the increased plasma glucose (PG) and decreased insulin (INS) in HFD-STZ rats[4].
| Animal Model: | Rats[1]. |
| Dosage: | 0.1-3 mg/kg. |
| Administration: | P.O.. |
| Result: | Significantly increased the number of shocks that rats received. Significantly increased the time spent in the light compartment but only slightly increased that time at 0.03 mg/kg, p.o. (P<0.1). |
storage
Store at +4°C
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