Overview
Alomone Labs is pleased to offer the nAChR Agonist Explorer Kit (#EK-204). This Explorer Kit includes nAChR agonists, ideal for screening purposes.
Compounds
| Product Name | Cat # | 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 |
(-)-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 |
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.
- Kombo, D.C. et al. (2011) Eur. J. Med. Chem. 46, 5625.
- Albuquerque, E.X. et al (2009) Physiol. Rev. 89, 73.
- Kalamida, D. et al. (2007) FEBS J. 274, 3799.
- Karlin, A. et al. (1986) Ann. NY. Acad. Sci. 463, 53.
