Butinazocine
Butinazocine is a benzomorphan derivative and is a mixed agonist–antagonist at opioid receptors, being a kappa-partial agonist and mu-antagonist. It has analgesic effects and can induce dysphoria, a state of unease or generalized dissatisfaction with life.
Chemistry[edit | edit source]
Butinazocine is chemically classified as a benzomorphan, a class of opioids that are structurally related to morphine. The benzomorphans are a group of morphinan-based compounds that do not contain a basic nitrogen atom in the morphinan skeleton itself, unlike most other opioids.
Pharmacology[edit | edit source]
Butinazocine acts as a mixed agonist–antagonist at opioid receptors. It is a partial agonist at the kappa opioid receptor and an antagonist at the mu opioid receptor. The kappa opioid receptor is involved in mediating the effects of opioids on mood, consciousness, motor control, and the perception of pain, while the mu opioid receptor is involved in mediating the effects of opioids on analgesia, respiratory depression, and euphoria.
Clinical significance[edit | edit source]
The analgesic effects of butinazocine can be useful in the management of pain. However, its ability to induce dysphoria can limit its clinical usefulness. Dysphoria is a state of unease or generalized dissatisfaction with life, which can be a significant side effect of kappa opioid receptor activation.
See also[edit | edit source]
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Contributors: Prab R. Tumpati, MD