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L-741626

Catalog No. T15686 CAS 81226-60-0

Synonyms: 3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole

L-741626 (3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole) is a selective antagonist of D2 dopamine receptor (Ki: 2.4, 100, and 220 nM for human D2, D3 and D4 receptors respectively).

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L-741626, CAS 81226-60-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 80.00
25 mg	In stock	$ 156.00
50 mg	In stock	$ 289.00
100 mg	In stock	$ 463.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 98.9%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	L-741626 (3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole) is a selective antagonist of D2 dopamine receptor (Ki: 2.4, 100, and 220 nM for human D2, D3 and D4 receptors respectively).
Targets&IC50	D2 receptor (human):(ki)2.4 nM, D3 receptor (human):100 nM(ki), D4 receptor (human):220 nM(ki)
In vitro	L-741626 is an effective antagonist (EC50 (D2)=4.46 nM) with some D2 selectivity (EC50 (D3)=90.4 nM), in the functional assay. L-741626 is prepared by literature methods (Ki (D2)=11.2 nM). L-741626 also shows a D3/D2 and D4/D2 selectivity ratio of 15-fold and 136-fold, respectively. Intrinsic activities using inhibition of quinpirole stimulation of mitogenesis in human dopamine D2 or D3 receptors transfected into Chinese hamster ovary (CHO) cells, in a functional assay [2].
In vivo	In pramipexole-trained male Sprague Dawley rats, L-741626 (1.0 mg/kg; i.h.) is effective at shifting to the right the pramipexole dose-response curve [3]. Coadministration Cocaine with the D2 antagonist L-741626 (3 mg/kg; i.p.; 15 min before Cocaine) for 5 days decreases the Cocaine-induced enhance in microglial TNF-α production in adult mice [4].

Synonyms	3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole
Molecular Weight	340.85
Formula	C20H21ClN2O
CAS No.	81226-60-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 40 mg/mL (117.35 mM), Sonification is recommended.

References and Literature

1. Lewitus GM, et al. Microglial TNF-α Suppresses Cocaine-Induced Plasticity and Behavioral Sensitization. Neuron. 2016 May 4;90(3):483-91. 2. Grundt P, et al. Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR. Bioorg Med Chem Lett. 2007 Feb 1;17(3):745-9. 3. Koffarnus MN, et al. The discriminative stimulus effects of dopamine D2- and D3-preferring agonists in rats. Psychopharmacology (Berl). 2009 Apr;203(2):317-27. 4. Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Neurotransmitter Receptor Compound Library NO PAINS Compound Library Bioactive Compound Library Natural Product Library for HTS RO5 Drug-like Natural Product Library Anti-Parkinson's Disease Compound Library Natural Product Library

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Keywords

L-741626 81226-60-0 GPCR/G Protein Neuroscience Dopamine Receptor L 741626 receptor selective TNF-α Inhibitor dopamine production 3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole L741626 inhibit inhibitor

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