Tebanicline

Tebanicline (also known as ABT-594) is a synthetic organic compound and a potent analgesic drug that was developed by the pharmaceutical company Abbott Laboratories. It is structurally related to the natural alkaloid epibatidine, which is found in the skin of certain species of poison dart frogs.

Chemistry

Tebanicline is a nicotinic acetylcholine receptor (nAChR) agonist. It is structurally similar to epibatidine, but it has been modified to reduce its toxicity and increase its therapeutic index. The chemical formula of tebanicline is C16H20N2O.

Pharmacology

Tebanicline acts as a potent analgesic by binding to and activating the α4β2 subtype of the nAChR. This receptor subtype is found in the central nervous system and is involved in pain perception. Activation of the α4β2 nAChR by tebanicline leads to an increase in the release of various neurotransmitters, including dopamine, serotonin, and norepinephrine, which can help to alleviate pain.

Clinical Development

Tebanicline was initially developed as a potential treatment for chronic pain and neuropathic pain. However, its development was discontinued in phase II clinical trials due to adverse side effects, including nausea and vomiting.

Side Effects

The most common side effects of tebanicline include nausea, vomiting, and dizziness. These side effects were the primary reason for the discontinuation of its clinical development.

See Also

• Epibatidine
• Nicotinic acetylcholine receptor
• Abbott Laboratories

References

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