| Identification | Back Directory | [Name]
NS3861 >=98% (HPLC) | [CAS]
216853-59-7 | [Synonyms]
NS3861 >=98% (HPLC)
8-Azabicyclo[3.2.1]oct-2-ene, 3-(3-bromo-2-thienyl)-8-methyl-
α3β4 nAChR,inhibit,NS 3861,Inhibitor,NS3861,Heteromeric,Patch Clamp,Nicotinic acetylcholine receptors,nAChR,NS-3861,Pharmacology | [Molecular Formula]
C12H14BrNS | [MDL Number]
MFCD30182246 | [MOL File]
216853-59-7.mol | [Molecular Weight]
284.22 |
| Chemical Properties | Back Directory | [Boiling point ]
358.5±42.0 °C(Predicted) | [density ]
1.456±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
8.26±0.40(Predicted) | [color ]
Off-white to light yellow | [InChIKey]
ZJCNRVHZJADROC-UHFFFAOYSA-N | [SMILES]
BrC1=C(SC=C1)C2=CC(N3C)CCC3C2 |
| Hazard Information | Back Directory | [Uses]
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively[1]. | [Biological Activity]
NS3861 is a neuronal nicotinic receptor agonist th at selectively activates α3 containing nAChRs and it displays higher efficacy at the α3β2 receptor compared with the α3β4 receptor. NS3861 does not activate α4 containing receptors. NS3861 was reported to reverse chronic opioid-induced constipation in vivo. | [References]
[1] Kasper Harps?e, et al. Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors. J Biol Chem. 2013 Jan 25;288(4):2559-70. DOI:10.1074/jbc.M112.436337 |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|