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VU0152100

Cat. No. M8848
VU0152100 Structure
Synonym:

VU152100

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Biological Activity

Positive allosteric modulator of muscarinic choline receptor M4. Potentiates activation by acetylcholine, but posesses no intrinsic agonist activity alone.

Chemical Information
Molecular Weight 341.43
Formula C18H19N3O2S
CAS Number 409351-28-6
Solubility (25°C) DMSO: ≥50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Alberto Brugnoli, et al. Striatal and nigral muscarinic type 1 and type 4 receptors modulate levodopa-induced dyskinesia and striato-nigral pathway activation in 6-hydroxydopamine hemilesioned rats

[2] Paulina Cieślik, et al. Simultaneous activation of muscarinic and GABA B receptors as a bidirectional target for novel antipsychotics

[3] Kevin Stoll, et al. Effects of muscarinic M 1 and M 4 acetylcholine receptor stimulation on extinction and reinstatement of cocaine seeking in male mice, independent of extinction learning

[4] Nellie E Byun, et al. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100

[5] Ditte Dencker, et al. An allosteric enhancer of M₄ muscarinic acetylcholine receptor function inhibits behavioral and neurochemical effects of cocaine

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