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VU 0255035 is a M1 muscarinic acetylcholine receptor (mAChR) antagonist (Ki = 14.87 nM). VU 0255035 shows higher selectivity to the M1 orthosteric site than other receptor subtypes. The M(1) mAChR is of particular interest as a potential target for treatment of CNS disorders. Whole-cell patch-clamp recordings demonstrate that VU0255035 inhibits potentiation of N-methyl-D-aspartate receptor currents by the muscarinic agonist carbachol in hippocampal pyramidal cells. VU0255035 has excellent brain penetration in vivo and is efficacious in reducing pilocarpine-induced seizures in mice. VU 0255035 does not induce the severe cognitive deficits seen with nonselective mAChR antagonists and could provide a novel approach for the treatment certain of CNS disorders.
| Molecular Weight | 432.52 |
| Formula | C18H20N6O3S2 |
| CAS Number | 1135243-19-4 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related AChR/AChE Products |
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| SVT-40776
SVT-40776 is a novel M3 muscarinic receptor antagonist. |
| Aniracetam
Aniracetam is a compound that promotes intellectual development and neuroprotection. |
| Biperiden hydrochloride
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. |
| Levetiracetam
Levetiracetam (UCB L059) is an antiepileptic, it is also a selective M2 muscarinic acetylcholine receptors (mAChR) inhibitor. |
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