Cys-loop, cationic

Nicotinergic acetylcholine receptors are made up of 5 subunits, symmetrically arranged around a central pore (ion channel). It is considered the best-characterized LGIC and a prototypical structure for the class of 4TM receptors. nAChRs are found mainly in postsynaptic membranes of central nervous system synapses and of the neuromuscular endplate. The physiological signal to which nAChR responds is the neurotransmitter acetylcholine, but it is also activated by nicotine. The assembly of combinations of subunits (17 distinct subunits have been identified) results in a large number of different receptors with a high variety of functional diversity as a result[1]. 5-HT3 differ from all other 5-HT (serotonin) receptors whose actions are mediated via G proteins. Their structure and function has placed them in the Cys-loop family of cationic ligand-gated ion channels. 5-HT3 receptors are located in both the peripheral (PNS) and central (CNS) nervous systems. In the CNS, 5-HT3 receptors may play roles in a variety of functions including emesis, cognition and anxiety, whereas in the PNS they play a role in a variety of sympathetic, parasympathetic and sensory functions (e.g. signaling in gastrointestinal tract, gut motility and peristalsis)[2].


[1] Ligand-Gated Ion Channels. F. Hucho, C. Weise. Angew.Chem.Int.Ed. 2001, 40, 3100-3116.
[2] 5-HT3 Receptors. A. J. Thompson, S. C. R. Lummis. Curr Pharm Des. 2006; 12(28): 3615–3630.

14 Item(s)

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Axon ID Name Description From price
1097 Alosetron hydrochloride 5-HT3 antagonist €85.00
2401 AT 1001 High affinity and selective α3β4 nAChR ligand with partial agonistic and antagonistic effects €95.00
1096 Azasetron hydrochloride 5-HT3 antagonist €90.00
2534 Azasetron hydrochloride, (+)- 5-HT3 antagonist €135.00
2535 Azasetron hydrochloride, (-)- 5-HT3 antagonist €135.00
1153 B-HT 920 dihydrochloride D2 agonist, α2 adrenoceptor agonist; 5-HT3 antagonist €75.00
1077 Epibatidine dihydrochloride, (+)- Nicotinic acetylcholine receptor agonist €155.00
1078 Epibatidine dihydrochloride, (-)- Nicotinic acetylcholine receptor agonist €155.00
1076 Epibatidine dihydrochloride, (±)- Nicotinic acetylcholine receptor agonist €95.00
2621 GAT107 allosteric agonist and PAM of α7 nAChR  Recently added €105.00
1449 Granisetron hydrochloride 5-HT3 antagonist €85.00
2109 PHA 543613 dihydrochloride nAChR agonist (α7 sub-unit selective) €85.00
1384 Varenicline dihydrochloride Nicotinic acetylcholine receptor agonist €95.00
2074 Varenicline tartrate Selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist €95.00

14 Item(s)

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