R-VK4-40

R-VK4-40 is a highly selective and potent dopamine D3 receptor antagonist, developed as a potential therapy for opioid use disorder and pain management. Preclinical studies demonstrate R-VK4-40’s ability to attenuate the rewarding effects of oxycodone and cocaine, reduce opioid self-administration, and enhance opioid-induced analgesia without compromising analgesic efficacy or inducing significant unwanted effects, such as cardiovascular side effects or locomotor disruption. R-VK4-40 displays excellent brain penetration after oral administration and has shown safety in animal models. It is under investigation for use in substance use disorders, specifically opioid and cocaine addiction, and pain, with a focus on reducing reward-driven drug-seeking and relapse, while potentially allowing for lower opioid dosing to decrease dependence and tolerance[1][3][4][5][8][9].

Other names

N-[(3R)-4-[4-(2-chloro-3-ethylphenyl)-1-piperazinyl]-3-hydroxybutyl]-1H-indole-2-carboxamide