nAChR Agonist Explorer Kit

A Screening Package of nAChR Activators Economically Priced
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
Cat #: EK-204
Sizes: 9 Vials
Last update: 03/09/2018

Alomone Labs is pleased to offer the nAChR Agonist Explorer Kit (#EK-204). This Explorer Kit includes nAChR agonists, ideal for screening purposes.

For research purposes only, not for human use
Compounds
Product NameCat #Size
1,1-Dimethyl-4-phenylpiperazinium iodide
D-125 1 x 1 g
(-)-Cytisine
C-130 1 x 10 mg
DMAB-anabaseine dihydrochloride
D-110 1 x 5 mg
Ivermectin
I-110 1 x 250 mg
(-)-Nicotine ditartrate
N-175 1 x 1 g
PNU-120596
P-350 1 x 10 mg
PNU 282987
P-110 1 x 5 mg
RJR 2403 oxalate
R-115 1 x 5 mg
Varenicline tartrate
V-105 1 x 5 mg
References
Scientific Background

Acetylcholine, released by cholinergic neurons, activates two groups of acetylcholine receptors (AChRs); muscarinic AChRs (mAChRs) which belong to the superfamily of G-protein coupled receptors (GPCRs) and nicotinic AChRs (nAChRs) which belong to the ligand-gated ion channel superfamily. nAChRs also respond to nicotine, hence their name1.

To date, 17 different, but related, subunits of nAChRs have been identified and cloned. They consist of α subunits (α1-10), which are responsible for the binding of ligands. In fact, this subunit includes a Cys-loop in the first extracellular domain that is required for agonist binding2. The other subunits responsible for making up the active receptor are the β (β1-4), γ, δ and ε subunits3. Structurally, all subunits have the following: a conserved large extracellular N-terminal domain, 3 conserved transmembrane domains, a variable cytoplasmic loop and a fourth transmembrane domain with a short extracellular C-terminal domain.  An active nAChR is generally a heteropentamer of these various subunits organized around a central pore1.

nAChRs are validated therapeutic targets for various CNS pathologies4.

References
  1. Kombo, D.C. et al. (2011) Eur. J. Med. Chem. 46, 5625.
  2. Albuquerque, E.X. et al (2009) Physiol. Rev. 89, 73.
  3. Kalamida, D. et al. (2007) FEBS J. 274, 3799.
  4. Karlin, A. et al. (1986) Ann. NY. Acad. Sci. 463, 53.
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