Overview
Alomone Labs is pleased to offer the nAChR Antagonist Explorer Kit (#EK-205). This Explorer Kit includes nAChR antagonists, ideal for screening purposes.
Compounds
| Product Name | Cat # | Size |
|---|---|---|
Azemiopsin |
STA-100 | 1 x 0.1 mg |
α-Bungarotoxin |
B-100 | 1 x 0.5 mg |
αA-Conotoxin OIVA |
STC-520 | 1 x 10 µg |
αA-Conotoxin PIVA |
STC-600 | 1 x 50 µg |
αC-Conotoxin PrXA |
STC-620 | 1 x 0.1 mg |
α-Conotoxin AuIA |
STC-960 | 1 x 0.25 mg |
α-Conotoxin AuIB |
STC-310 | 1 x 0.1 mg |
α-Conotoxin EI |
STC-900 | 1 x 0.1 mg |
α-Conotoxin GI |
STC-500 | 1 x 0.5 mg |
α-Conotoxin ImI |
C-290 | 1 x 0.1 mg |
α-Conotoxin LtIA |
STC-550 | 1 x 0.5 mg |
α-Conotoxin MI |
STC-370 | 1 x 0.1 mg |
α-Conotoxin PeIA |
STC-970 | 1 x 0.1 mg |
α-Conotoxin PIA |
STC-870 | 1 x 0.1 mg |
Huwentoxin-I |
STH-050 | 1 x 0.1 mg |
(-)-Lobeline hydrochloride |
L-120 | 1 x 100 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 is 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.
