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Varenicline (CP 526555) is a selective α4β2 nicotinic receptor partial agonist, it stimulates nicotine receptors more weakly than nicotine itself does. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | MS/DB neurons |
| Preparation method | In one subset of experiments, bath solution containing nicotine (10 μM) was initially applied followed by a nicotine (10 μM) plus varenicline (10 μM) bath solution. For a second subset of experiments, the order of drug application was reversed with a varenicline (10 μM) containing bath solution applied first followed by a varenicline (10 μM) plus nicotine (10 μM) bath solution. |
| Concentrations | 10 μM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague–Dawley rats |
| Formulation | saline |
| Dosages | 0.5, 1, 2 and 3 mg/kg |
| Administration | s.c. |
| Molecular Weight | 211.26 |
| Formula | C13H13N3 |
| CAS Number | 249296-44-4 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related AChR/AChE Products |
|---|
| AT 1001
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) with Ki of 2.64 nM. |
| Dihydro-β-erythroidine hydrobromide
Dihydro-β-erythroidine hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. |
| Spinosad
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. |
| TAE-1
TAE-1 is a potent inhibitor of AChE and BuChE. |
| PE154
PE154 is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively). |
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