Selective, high affinity negative modulator of AMPA receptors containing TARP-γ8
JNJ 55511118 is a high affinity and selective negative modulator of AMPA receptors containing TARP-γ8 (Ki = 26 nM). Exhibits <50% binding against a panel of 52 receptors, ion channels and transporters (except 5HT2B and melatonin receptors 78% and 57%, respectively). Also displays minimal activity against other TARP-less AMPARs and AMPARs coexpressed with other TARPs or CNIH2. It reduces alcohol self-administration in a mouse models of chronic drinking. Orally bioavailable and brain penetrant. Anticonvulsant.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-125341 |
| Réf. fabricant | 18719817 |
| Nom chimique ou matériau | 5-[2-Chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydro-2H-benzimidazol-2-one |
| CAS | 2036081-86-2 |
| Plage de pourcentage du dosage | >98% |
| Quantité | 25 mg |
| Formule moléculaire | C<sub>14</sub>H<sub>8</sub>ClF<sub>3</sub>N<sub>2</sub>O<sub>2</sub> |
| Poids de la formule | Observed MW: 328.67 |
