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
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
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
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).
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