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A-381393

Cat. No. M11167
A-381393  Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 240  USD240 In stock
25mg USD 430  USD430 In stock
50mg USD 600  USD600 In stock
100mg USD 880  USD880 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

A-381393 IS AN EFFECTIVE, SELECTIVE, AND BLOOD-BRAIN BARRIER-PERMEABLE dopamine D4 receptor Antagonist, dopamine D for humans4.4,D4.2 AND D4.7 receptors Ki The values are 1.5, 1.9, and 1.6 nM, respectively, with selectivity being D1,D2,D3,D5 MORE THAN 2700 TIMES THE DOPAMINE RECEPTOR. A-381393 VS. 5-HT2A MODERATE SELECTIVITY, Ki The value is 370 nM.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 320.43
Formula C20H24N4
CAS Number 726174-00-1
Purity >99%
Solubility DMSO ≥ 40 mg/mL
Storage at -20°C
References

[1] Danuta Marona-Lewicka, et al. Behav Pharmacol. WAY 100635 produces discriminative stimulus effects in rats mediated by dopamine D(4) receptor activation

[2] Danuta Marona-Lewicka, et al. Psychopharmacology (Berl). Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI

[3] Robert S Bitner, et al. Neuropharmacology. Dopamine D4 receptor signaling in the rat paraventricular hypothalamic nucleus: Evidence of natural coupling involving immediate early gene induction and mitogen activated protein kinase phosphorylation

[4] Masaki Nakane, et al. Neuropharmacology. 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist

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