Drug intelligence / Profile preview

cyprenorphine

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous (primarily For Veterinary Use)
01

Overview

Cyprenorphine is a synthetic opioid compound and a derivative of the morphinan class. It acts as a highly potent mixed agonist–antagonist at opioid receptors. Cyprenorphine is primarily known for its strong antagonistic activity at opioid receptors—blocking the effects of opioids such as morphine and etorphine—and is roughly 35 times more potent than nalorphine as an antagonist. While it has some agonist properties similar to buprenorphine and diprenorphine (to which it is structurally related), cyprenorphine produces pronounced dysphoric and hallucinogenic effects that limit its use in humans. Its main application has been in veterinary medicine to reverse the immobilizing effects of etorphine in large animals after procedures. The drug induces psychotomimetic side effects in humans and has no accepted medical use due to safety concerns[1][2][4][5].

Brand names
none
Other names
CiprenorfinaCyprenorphinum6,14-Ethenomorphinan-7-methanol 17-(cyclopropylmethyl)-4,5-epoxy-3-hydroxy-6-methoxy-a,a-dimethyl-(5a,7a)-(5a,7a)-17-(Cyclopropylmethyl)-4,5-epoxy-3-hydroxy-6-methoxy-a,a-dimethyl-6,14-ethenomorphinan-7-methanol
02

Targets

DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)

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