Free shipping on all orders over $ 500

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
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

Chemical Information
Molecular Weight 320.43
Formula C20H24N4
CAS Number 726174-00-1
Solubility (25°C) DMSO ≥ 40 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] 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

Related Dopamine Receptor Products
SV 156

SV 156 is a potent and selective D2 dopamine receptor antagonist, with a Ki of 2.5 nM for hD2. SV 156 has approximately 40-fold binding selectivity for D2 dopamine receptors compared to the D3 receptor subtype.

Cyclo(glycyl-L-leucyl)

Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity.

Onzigolide

Onzigolide (BIM-23A760), a chimeric dopamine-somatostatin compound, shows potent agonist activity at both DA type 2 (D2R) and SST type 2 (SSTR2) receptors.

CVL-871

CVL-871 is a partial agonist at dopamine D1/5 receptors and may be used in dementia-related studies.

Paliperidone palmitate

Paliperidone palmitate is the ester precursor compound of Paliperidone, a potent dopamine antagonist and 5-HT2A antagonist. Paliperidone is a potent dopamine antagonist and 5-HT2A antagonist.

  Catalog
Abmole Inhibitor Catalog




Keywords: A-381393 supplier, Dopamine Receptor, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.