Bionomics' lead drug candidate BNC210, currently in Phase 2 for the treatment of generalized anxiety disorder, is a novel, proprietary negative allosteric modulator of the alpha-7 nicotinic acetylcholine receptor
The IRAC mode of action groups to which the above insecticides belong are as follows: fipronil (2B, GABA-gated chloride channel antagonists), lambda-cyhalothrin (3A, Sodium channel modulators), imidacloprid, thiacloprid and thiamethoxam (4A, Nicotinic acetylcholine receptor
[nAChR] agonists), and spinosad (5, Nicotinic acetylcholine receptor
[nAChR] allosteric activators).
Varenicline, an a4ss2 nicotinic acetylcholine receptor
partial agonist, vs sustained-release bupropion and placebo for smoking cessation.
Selective changes in nicotinic acetylcholine receptor
subtypes related to tobacco smoking: an immuno-histochemical study.
Varenicline is pharmacologically known as an alpha4beta2 nicotinic acetylcholine receptor
partial agonist, which means that it activates the brain's nicotinic receptors in a manner similar to nicotine, but with less affinity (effect).
Inclusion of alpha-bungarotoxin, a nicotinic acetylcholine receptor
antagonist, or cycloheximide, a protein synthesis inhibitor, during nicotine treatment abolished nicotine-induced podosome rosette formation in the rat cells, suggesting that signalling through the nicotinic acetylcholine receptors
and synthesis of new proteins are required for podosome rosette formation.
dorsalis, we report the cloning and characterization of the nicotinic acetylcholine receptor
alpha6 cDNA and the expression patterns at different developmental stages and in different tagmata of adult flies using quantitative real-time PCR.
Nicotine acts on the brain by directly binding to and activating a molecule called the nicotinic acetylcholine receptor
, which is found on certain brain cells.
Like snake venom, Syn-ake acts as an antagonist of the muscle nicotinic acetylcholine receptor
, blocking Na+ release at the post--synaptic membrane, and inhibiting muscle contraction.
The antigenic target is the nicotinic acetylcholine receptor
(nAChR) of skeletal muscles.
EnVivo's lead product is an alpha-7 nicotinic acetylcholine receptor
agonist that has successfully completed Phase 2b clinical trials in both schizophrenia and Alzheimer's disease.
Cytisine is a partial agonist that binds with high affinity to a subtype of the nicotinic acetylcholine receptor
, which is also the primary target of the smokingcessation drug varenicline.