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WAY-100135 dihydrochloride

Cat. No. M8856
WAY-100135 dihydrochloride Structure
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Biological Activity

WAY-100135 dihydrochloride is a potent, selective 5-HT1A receptor antagonist (IC50 = 15 nM). It is selective over 5-HT1B, 1C, 2,α1, α2 and D2 receptors (IC50 > 1000 nM).

Chemical Information
Molecular Weight 468.46
Formula C24H33N3O2 · 2HCl
CAS Number 149055-79-8
Solubility (25°C) Water: ≥10 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] E A Del Bel, et al. Role of nitric oxide on motor behavior

[2] W Lscher, et al. Effects of the novel 5-HT1A receptor antagonist, (+)-WAY 100135, on stereotyped behaviour induced by the NMDA receptor antagonist dizocilpine in rats

[3] R J Rodgers, et al. Anxiolytic-like effect of (S)-WAY 100135, a 5-HT1A receptor antagonist, in the murine elevated plus-maze test

[4] C Routledge, et al. Differential effects of WAY-100135 on the decrease in 5-hydroxytryptamine release induced by buspirone and NAN-190

[5] M Carli, et al. (S)-WAY 100135, a 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine

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