Selective positive allosteric modulator of M4 receptors.
LY 2033298 is a selective positive allosteric modulator of M4 receptor (KB = 200 nM, α = 35); increases the potency of acetylcholine by 40-fold. Exhibits no effect at hM1/3/5 receptors and a small effect at hM2 (KB = 1 μM α = 3.7). Potentiates other full and partial orthosteric agonists, including Carbachol, Oxotremorine-M, and McN-A343 . Does not affect binding of antagonist NMS. Active
in vivo
. Antipsychotic.
α indicates the degree of allosteric enhancement when both orthosteric and allosteric sites are occupied (derived from the allosteric ternary complex model).
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-151452 |
| Réf. fabricant | 18729376 |
| Nom chimique ou matériau | 3-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide |
| CAS | 886047-13-8 |
| Quantité | 25 mg |
| Formule moléculaire | C<sub>13</sub>H<sub>14</sub>ClN<sub>3</sub>O<sub>2</sub>S |
| Pureté | 98% |
