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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 |
|---|
| AT 1001
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) with Ki of 2.64 nM. |
| Dihydro-β-erythroidine hydrobromide
Dihydro-β-erythroidine hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. |
| Spinosad
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. |
| TAE-1
TAE-1 is a potent inhibitor of AChE and BuChE. |
| PE154
PE154 is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively). |
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