Tebanicline is a drug developed by Abbott

Abbott Laboratories

Abbott Laboratories is an American-based global, diversified pharmaceuticals and health care products company. It has 90,000 employees and operates in over 130 countries. The company headquarters are in Abbott Park, North Chicago, Illinois. The company was founded by Chicago physician, Dr....

, which acts as a partial agonist

Partial agonist

Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...

 at neuronal nicotinic acetylcholine receptor

Nicotinic acetylcholine receptor

Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction...

s, binding to both the α3β4

Ganglion type nicotinic receptor

The ganglion type nicotinic receptor is a type of nicotinic acetylcholine receptor, consisting of the subunit combination 23.It is located in the autonomic ganglia, where activation yields EPSP, mainly by increased Na+ and K+ permeability....

 and the α4β2

Alpha-4 beta-2 nicotinic receptor

The alpha-4 beta-2 nicotinic receptor, also known as the α4β2 receptor, is a type of nicotinic acetylcholine receptor, consisting of α4 and β2 subunits...

 subtypes. It was developed as a less toxic analogue of the potent frog-derived compound epibatidine

Epibatidine

Epibatidine is an alkaloid found on the skin of the endangered Ecuadorian frog, Epipedobates tricolor. These frogs, like other poison dart frogs, are best known for their ability to sequester poisons from their prey and secrete these poisons onto their backs. Many Amerindian tribes would swipe the...

, which is some 200x stronger than morphine

Morphine

Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...

 as an analgesic

Analgesic

An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....

 but produces extremely dangerous toxic side effects. Like epibatidine, tebanicline showed potent analgesic activity against neuropathic pain

Neuropathic pain

Neuropathic pain results from lesions or diseases affecting the somatosensory system. It may be associated with abnormal sensations called dysesthesia, which occur spontaneously and allodynia that occurs in response to external stimuli. Neuropathic pain may have continuous and/or episodic ...

in both animal and human trials, but with far less toxicity than its parent compound.

Tebanicline got as far as Phase II trials in humans, but was dropped from further development due to unacceptable incidence of gastrointestinal side effects. However further research in this area is ongoing, and it is expected that development of new neural nicotinic acetylcholine receptor agonists will be likely to lead to novel analgesics suitable for use in humans within the next few years.