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Merck
CN

SML2881

R-VK4-40

≥98% (HPLC)

Synonym(s):

R-VK4-40, N-[(3R)-4-[4-(2-Chloro-3-ethylphenyl)-1-piperazinyl]-3-hydroxybutyl]-1H-indole-2-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C25H31ClN4O2
CAS Number:
2133454-52-9
Molecular Weight:
454.99
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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InChI

1S/C25H31ClN4O2/c1-2-18-7-5-9-23(24(18)26)30-14-12-29(13-15-30)17-20(31)10-11-27-25(32)22-16-19-6-3-4-8-21(19)28-22/h3-9,16,20,28,31H,2,10-15,17H2,1H3,(H,27,32)/t20-/m1/s1

InChI key

OIRZLTZLOKARTG-HXUWFJFHSA-N

SMILES string

O=C(C1=CC2=C(C=CC=C2)N1)NCC[C@H](CN3CCN(C4=CC=CC(CC)=C4Cl)CC3)O

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

R-VK4-40 is an orally available, highly selective and potent dopamine D3 receptor (D3R) antagonists that does not exhibit unwanted cardiovascular effects. R-VK4-40 attenuates oxycodone induced rewards without compromising antinociceptive effects in rats. It reduces oxycodone self-administration and suppress naloxone-caused opioid withdrawal.
orally available, highly selective and potent dopamine D3 receptor (D3R) antagonists that does not exhibit unwanted cardiovascular effects

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000131251
0000131250
0000127296

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Anver Basha Shaik et al.
Journal of medicinal chemistry, 62(20), 9061-9077 (2019-09-19)
Dopamine D3 receptors (D3R) play a critical role in neuropsychiatric conditions including substance use disorders (SUD). Recently, we reported a series of N-(3-hydroxy-4-(4-phenylpiperazin-1-yl)butyl)-1H-indole-2-carboxamide analogues as high affinity and selective D3R lead molecules for the treatment of opioid use disorders (OUD).
Chloe J Jordan et al.
Neuropharmacology, 158, 107597-107597 (2019-04-12)
Prescription opioid abuse is a global crisis. New treatment strategies for pain and opioid use disorders are urgently required. We evaluated the effects of R-VK4-40, a highly selective dopamine (DA) D3 receptor (D3R) antagonist, on the rewarding and analgesic effects
Chloe J Jordan et al.
The Journal of pharmacology and experimental therapeutics, 371(3), 602-614 (2019-09-29)
Opioid and cocaine abuse are major public health burdens. Existing medications for opioid use disorder are limited by abuse liability and side effects, whereas no treatments are currently approved in the United States for cocaine use disorder. Dopamine D3 receptor

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