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Product Feature - Nicotinic Receptors
nAChRs in skeletal muscle have been characterised in detail whereas mammalian neuronal nAChRs in the central nervous system have more recently become the focus of intense research efforts. This was fuelled by the realisation that nAChRs in the brain and spinal cord are potential therapeutic targets for a range of neurological and psychiatric conditions.The generation of transgenic mice with deleted or mutated nAChR subunits and the development of subtype-ligands to complement the generous armamentarium of natural products that target nAChRs, support this research. Progress is being made in understanding the physiological roles of nAChRs in the brain and the underlying molecular and cellular mechanisms, and the contribution of nAChRs to pathological conditions.
Extract taken from Tocris' latest review on nicotinic ACh receptors written by a leading researcher in the field, Sue Wonnacott.
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Key nicotinic receptor compounds now available from Tocris include:
Selective partial agonist at α4β2 receptors
2737 l TC 2559
Displays selectivity for (α4)2(β2)3 receptor stoichiometry and enhanced CNS-PNS selectivity ratio. Attenuates scopolamine-induced cognitive deficits in a step-through passive avoidance task.
Related Products: 5-Iodo-A-85380 Dihydro-β-erythroidine RJR 2403
TC 2559 RJR 2403
α4β2 0.18 0.026
α4β4 12.5 -
α2β4 14.0 -
α3β4 >30 >1000
α1β1γ1 - >1000
α3β2 >100 15
α7 >100 36(Ki)
EC50 values (in μM).
Selective α7 nAChR agonist
2303 l PNU 282987
Ki = 26 nM.   Displays  negligible  blockade  of  α1β1γδ  and  α3β4  nAChRs
(IC50 = 60 μM). Found to be inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM).
Related Products: PNU 120596 DMAB-anabaseine
α7 neuronal nicotinic receptor antagonist
1029 l Methyllycaconitine
Ki = 1.4 nM. Interacts with α4β2 & α6β2 receptors at concentrations > 40 nM. Attenuates METH-induced neurotoxicity in mouse striatum in vivo.
Related Products: MG 624 α-Bungarotoxin
NEW Review
Neuronal nicotinic receptors review
Nicotinic ACh Receptors
Unique and Affordable New Screening Libraries
Tocriscreen Collections : For pricing and compound information click here
  • 1120 compounds
  • Pre-dissolved in DMSO
Tocriscreen Total (250 μL/well)
Tocriscreen Mini (50 μL/well)
More Nicotinic Receptor Compounds
Benzoquinonium
Nicotinic antagonist
(±)-Epibatidine
Very potent nicotinic agonist
Pancuronium
Nicotinic (neuromuscular) antagonist
(±)-Anatoxin A
Neuronal nicotinic agonist
Chlorisondamine
Nicotinic antagonist
Neuronal nAChR Role in CNS Disorders
Woodruff-Pak and Gould review the involvement of neuronal nAChRs in Alzheimer's disease and Schizophrenia (more)