A-381393 | CAS#726174-00-1 | dopamine D4 antagonist

A-381393
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531353

CAS#: 726174-00-1

Description: A-381393 is a potent and selective agonist of the dopamine D4 receptor. A-381393 potently bound to membrane from cells expressing recombinant human dopamine D4.4 receptor (Ki=1.5 nM), which was 20-fold higher than that of clozapine (Ki=30.4 nM). A-381393 exhibited highly selective binding for the dopamine D4.4 receptor (>2700-fold) when compared to D1, D2, D3 and D5 dopamine receptors.

Chemical Structure

A-381393

CAS# 726174-00-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531353
Name: A-381393
CAS#: 726174-00-1
Chemical Formula: C20H24N4
Exact Mass: 320.20
Molecular Weight: 320.440
Elemental Analysis: C, 74.97; H, 7.55; N, 17.48

Price and Availability

Size	Price	Availability
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: A-381393; A 381393; A381393;

IUPAC/Chemical Name: 2-[[4-(3,4-dimethylphenyl)piperazin-1-yl]methyl]-1H-benzimidazole

InChi Key: SAQMCVDGOIRQTC-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H24N4/c1-15-7-8-17(13-16(15)2)24-11-9-23(10-12-24)14-20-21-18-5-3-4-6-19(18)22-20/h3-8,13H,9-12,14H2,1-2H3,(H,21,22)

SMILES Code: CC1=CC=C(N2CCN(CC3=NC4=CC=CC=C4N3)CC2)C=C1C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	A-381393 is a brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors.
In vitro activity:	A-381393 binds to dopamine D4 receptor with nanomolar affinity (Ki = 1.5 nM), which is comparable with L-745870, and 36-fold higher than clozapine (Ki = 54 nM). A-381393 was more than 4000-fold selective for the dopamine D4 receptors as compared to dopamine D1, D2, D3 and D5 receptors. Reference: Neuropharmacology. 2005 Jul;49(1):112-21. https://pubmed.ncbi.nlm.nih.gov/15992586/
In vivo activity:	It has been demonstrated that the dopamine D4 receptor selective agonist PD168077 induces penile erection in conscious rats by centrally mediated mechanisms with an effective dose of 0.3 μmol/kg. To determine if A-381393 would attenuate this effect, the compound was dosed subcutaneously at 30 μmol/kg before administration of PD168077. When the percent incidence of penile erection was examined, PD168077 induced 75% incidence at the efficacious dose. In animals treated with A-381393, this incidence was significantly reduced to 48% (Fig. 7). Reference: Neuropharmacology. 2005 Jul;49(1):112-21. https://pubmed.ncbi.nlm.nih.gov/15992586/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	51.7	161.25

Preparing Stock Solutions

The following data is based on the product molecular weight 320.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Nakane M, Cowart MD, Hsieh GC, Miller L, Uchic ME, Chang R, Terranova MA, Donnelly-Roberts DL, Namovic MT, Miller TR, Wetter JM, Marsh K, Stewart AO, Brioni JD, Moreland RB. 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology. 2005 Jul;49(1):112-21. doi: 10.1016/j.neuropharm.2005.02.004. Epub 2005 Apr 1. PMID: 15992586.
In vitro protocol:	1. Nakane M, Cowart MD, Hsieh GC, Miller L, Uchic ME, Chang R, Terranova MA, Donnelly-Roberts DL, Namovic MT, Miller TR, Wetter JM, Marsh K, Stewart AO, Brioni JD, Moreland RB. 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology. 2005 Jul;49(1):112-21. doi: 10.1016/j.neuropharm.2005.02.004. Epub 2005 Apr 1. PMID: 15992586.
In vivo protocol:	1. Nakane M, Cowart MD, Hsieh GC, Miller L, Uchic ME, Chang R, Terranova MA, Donnelly-Roberts DL, Namovic MT, Miller TR, Wetter JM, Marsh K, Stewart AO, Brioni JD, Moreland RB. 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology. 2005 Jul;49(1):112-21. doi: 10.1016/j.neuropharm.2005.02.004. Epub 2005 Apr 1. PMID: 15992586.

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1: Marona-Lewicka D, Nichols DE. WAY 100635 produces discriminative stimulus effects in rats mediated by dopamine D(4) receptor activation. Behav Pharmacol. 2009 Feb;20(1):114-8. doi: 10.1097/FBP.0b013e3283242f1a. PubMed PMID: 19179855.

2: Marona-Lewicka D, Chemel BR, Nichols DE. Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI. Psychopharmacology (Berl). 2009 Apr;203(2):265-77. doi: 10.1007/s00213-008-1238-0. PubMed PMID: 18604600.

3: Bitner RS, Nikkel AL, Otte S, Martino B, Barlow EH, Bhatia P, Stewart AO, Brioni JD, Decker MW, Moreland RB. 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. Neuropharmacology. 2006 Apr;50(5):521-31. PubMed PMID: 16324724.

4: Nakane M, Cowart MD, Hsieh GC, Miller L, Uchic ME, Chang R, Terranova MA, Donnelly-Roberts DL, Namovic MT, Miller TR, Wetter JM, Marsh K, Stewart AO, Brioni JD, Moreland RB. 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology. 2005 Jul;49(1):112-21. PubMed PMID: 15992586.

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