Uses
VU0357017 is a subtype-selective M1 muscarinic acetylcholine allosteric agonist. VU0357017 has a potency of 200 nM and Achmax of 81% and had no activity at M2-M5 up to the highest concentrations tested and also had little or no detectable antagonist activity at any other mAChR subtype at concentrations over 2 orders of magnitude higher than those required to activate M1 or activity at a large panel of GPCRs, ion channels, and transporters. In contrast, TBPB inhibited responses to ACh at each of the other mAChR subtypes. VU0357017 was active in reversing cognitive deficits induced by Scopolamine (S200000) in a preclinical rodent model.
Uses
VU 0357017 Hydrochloride is a cholinergic M1 receptor antagonist and a cholinomimetic agent used for the treatment of behavioral and/or mental disorders.
Biological Activity
VU0357017 is a subtype-selective M1 muscarinic acetylcholine allosteric agonist. VU0357017 has a potency of 200 nM and Achmax of 81% and had no activity at M2-M5 up to the highest concentrations tested and also had little or no detectable antagonist activity at any other mAChR subtype at concentrations over 2 orders of magnitude higher than those required to activate M1 or activity at a large panel of GPCRs, ion channels, and transporters. In contrast, TBPB inhibited responses to ACh at each of the other mAChR subtypes. VU0357017 was active in reversing cognitive deficits induced by scopolamine in a preclinical rodent model.
in vivo
VU0357017 (1-10 mg/kg, i.p.) reverses scopolamine-induced disruption of the contextual fear conditioning response[2].
| Animal Model: | Male SpragueDawley rats (380-420 g) were pretreated with scopolamine[2] |
| Dosage: | 1, 3, 10 mg/kg |
| Administration: | A single i.p. |
| Result: | Produced a significant reversal of the scopolamine-induced deficits at a dose of 10 mg/kg. |
