Sazetidine A
Encyclopedia
Sazetidine A is a drug which acts as a subtype selective partial agonist
at α4β2
neural nicotinic acetylcholine receptor
s, acting as an agonist at (α4)2(β2)3 pentamers, but as an antagonist at (α4)3(β2)2 pentamers. It has potent analgesic
effects in animal studies comparable to those of epibatidine
, but with less toxicity, and also has antidepressant
action.
Partial agonist
Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...
at 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...
neural 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, acting as an agonist at (α4)2(β2)3 pentamers, but as an antagonist at (α4)3(β2)2 pentamers. It has potent 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 ....
effects in animal studies comparable to those of 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...
, but with less toxicity, and also has antidepressant
Antidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
action.