216853-60-0
216853-60-0 structure
- Name: NS3861
- Chemical Name: 3-(3-Bromo-2-thienyl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene (2E)-2-butenedioate (1:1)
- CAS Number: 216853-60-0
- Molecular Formula: C12H14BrNS.C4H4O4
- Molecular Weight: 400.287
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
- Create Date: 2020-01-11 16:09:51
- Modify Date: 2023-01-17 13:41:19
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A potent, subtype-selective α3β4 nAChR partial agonist with Ki of 0.62 nM; selectively activates receptors containing β4- but not β2-subunits, shows no efficacy at α4β2 receptors and only marginal efficacy at α4β4 receptors expressed in oocytes; enhances fecal pellet expulsion in a dose-dependent manner in mice that received long-term, but not short-term, morphine treatment.
| Name | 3-(3-Bromo-2-thienyl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene (2E)-2-butenedioate (1:1) |
|---|---|
| Synonyms |
3-(3-Bromo-2-thienyl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene (2E)-2-butenedioate (1:1)
8-Azabicyclo[3.2.1]oct-2-ene, 3-(3-bromo-2-thienyl)-8-methyl-, (2E)-2-butenedioate (1:1) |
| Description | A potent, subtype-selective α3β4 nAChR partial agonist with Ki of 0.62 nM; selectively activates receptors containing β4- but not β2-subunits, shows no efficacy at α4β2 receptors and only marginal efficacy at α4β4 receptors expressed in oocytes; enhances fecal pellet expulsion in a dose-dependent manner in mice that received long-term, but not short-term, morphine treatment. |
|---|---|
| References | References 1. Harpsøe K, et al. J Biol Chem. 2013 Jan 25;288(4):2559-70. 2. Gade AR, et al. J Pharmacol Exp Ther. 2016 Jun;357(3):520-8. View Related Products by Target nAChR |
| Molecular Formula | C12H14BrNS.C4H4O4 |
|---|---|
| Molecular Weight | 400.287 |
| Exact Mass | 399.013977 |