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p-MPPI hydrochloride 

Cat. No. M29350
p-MPPI hydrochloride  Structure
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Biological Activity

p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.

Chemical Information
Molecular Weight 578.87
Formula C25H28ClIN4O2
CAS Number 220643-77-6
Form Solid
Solubility (25°C) DMSO 17.86 mg/mL (ultrasonic)
Water 3.33 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, protect from light, dry, sealed
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] Vladimir S Naumenko, et al. Neurosci Lett. Central 5-HT3 receptor-induced hypothermia in mice: interstrain differences and comparison with hypothermia mediated via 5-HT1A receptor

[2] E Fiske, et al. Acta Physiol (Oxf). Increased extracellular 5-HT but no change in sleep after perfusion of a 5-HT1A antagonist into the dorsal raphe nucleus of rats

[3] P J Winsauer, et al. Behav Pharmacol. Differential effects of 5-HT agonists and antagonists on the repeated acquisition and performance of response sequences in monkeys

[4] B Ahlemeyer, et al. Eur J Pharmacol. The 5-HT1A receptor agonist Bay x 3702 inhibits apoptosis induced by serum deprivation in cultured neurons

[5] M B Shaikh, et al. Brain Res. Serotonin 5-HT1A and 5-HT2/1C receptors in the midbrain periaqueductal gray differentially modulate defensive rage behavior elicited from the medial hypothalamus of the cat

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Keywords: p-MPPI hydrochloride  supplier, 5-HT Receptor, inhibitors, activators

 
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