L-741,626
Modify Date: 2024-01-22 18:42:18
L-741,626 structure
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Common Name | L-741,626 | ||
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| CAS Number | 81226-60-0 | Molecular Weight | 340.84700 | |
| Density | 1.311g/cm3 | Boiling Point | 548.8ºC at 760 mmHg | |
| Molecular Formula | C20H21ClN2O | Melting Point | N/A | |
| MSDS | USA | Flash Point | 285.7ºC | |
Use of L-741,626L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively[1]. |
| Name | 4-(4-chlorophenyl)-1-(1H-indol-3-ylmethyl)piperidin-4-ol |
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| Synonym | More Synonyms |
| Description | L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively[1]. |
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| Related Catalog | |
| Target |
Ki: 2.4 nM (human D2 receptor), 100 nM (human D3 receptor), 220 nM (human D4 receptor)[1] |
| In Vitro | Intrinsic activities in a functional assay using inhibition of quinpirole stimulation of mitogenesis in human dopamine D2 or D3 receptors transfected into Chinese hamster ovary (CHO) cells, L-741626 is prepared by literature methods (Ki (D2)=11.2 nM) and displays a D3/D2 and D4/D2 selectivity ratio of 15-fold and 136-fold, respectively. In the functional assay L-741626 is a potent antagonist (EC50 (D2)=4.46 nM) with some D2 selectivity (EC50 (D3)=90.4 nM)[2]. |
| In Vivo | L-741626 (1.0 mg/kg; i.h.) is effective at shifting to the right the pramipexole dose-response curve in pramipexole-trained male Sprague Dawley rats[3]. Coadministrating Cocaine with the D2 antagonist L-741626 (3 mg/kg; i.p.; 15 min before Cocaine) for 5 days reduces the Cocaine-induced increase in microglial TNF-α production in adult mice[4]. |
| References |
| Density | 1.311g/cm3 |
|---|---|
| Boiling Point | 548.8ºC at 760 mmHg |
| Molecular Formula | C20H21ClN2O |
| Molecular Weight | 340.84700 |
| Flash Point | 285.7ºC |
| Exact Mass | 340.13400 |
| PSA | 39.26000 |
| LogP | 4.24280 |
| Index of Refraction | 1.686 |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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~%
L-741,626 CAS#:81226-60-0 |
| Literature: John Wyeth and Brother Limited Patent: US4358456 A1, 1982 ; |
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~95%
L-741,626 CAS#:81226-60-0 |
| Literature: Vangveravong, Suwanna; McElveen, Elizabeth; Taylor, Michelle; Xu, Jinbin; Tu, Zhude; Luedtke, Robert R.; Mach, Robert H. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 3 p. 815 - 825 |
| Precursor 3 | |
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| DownStream 0 | |
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Genome-wide shRNA screen revealed integrated mitogenic signaling between dopamine receptor D2 (DRD2) and epidermal growth factor receptor (EGFR) in glioblastoma.
Oncotarget 5(4) , 882-93, (2014) Glioblastoma remains one of the deadliest of human cancers, with most patients succumbing to the disease within two years of diagnosis. The available data suggest that simultaneous inactivation of cri... |
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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. 39 , 1941, (1996)
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The role of the dopamine D2 receptor in descending control of pain induced by motor cortex stimulation in the neuropathic rat.
Brain Res. Bull. 89(3-4) , 133-43, (2012) We studied in rats with a spinal nerve ligation-induced neuropathy whether dopamine D2 receptors (D2Rs) play a role in descending control of pain induced by stimulation of the primary motor cortex (M1... |
| 4-(4-Chlorophenyl)-1-(1H-indol-3-ylmethyl)-4-piperidinol |
| L 741,626 |
| 1-(indol-3-ylmethyl)-4-hydroxy-4-(p-chlorophenyl)piperidine |
| 4-Piperidinol,4-(4-chlorophenyl)-1-(1H-indol-3-ylmethyl) |
| 3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole |