951322-11-5
951322-11-5 structure
- Name: Desformylflustrabromine hydrochloride
- Chemical Name: 2-[6-Bromo-2-(2-methyl-3-buten-2-yl)-1H-indol-3-yl]-N-methylethan amine hydrochloride (1:1)
- CAS Number: 951322-11-5
- Molecular Formula: C16H22BrClN2
- Molecular Weight: 357.71600
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
- Create Date: 2016-12-22 00:05:16
- Modify Date: 2024-01-14 18:35:16
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Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
| Name | 2-[6-Bromo-2-(2-methyl-3-buten-2-yl)-1H-indol-3-yl]-N-methylethan amine hydrochloride (1:1) |
|---|---|
| Synonyms |
N-Methyllidocaine iodide
Deformylflustrabromine hydrochloride Desformylflustrabromine hydrochloride 6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride |
| Description | Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48. |
|---|---|
| Related Catalog | |
| Target |
α4β2 nAChR |
| In Vitro | Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48[1]. ACh-induced currents are potentiated and inhibited by Desformylflustrabromine hydrochloride in the high sensitivity (HS) and low sensitivity (LS) isoform preparations, although Desformylflustrabromine hydrochloride displays a higher potency on the LS isoform (pEC50=6.4±0.2) compare with the HS isoform (pEC50=5.6±0.2). Desformylflustrabromine hydrochloride potentiates ACh-induced responses of wild-type receptors expressed using the HS isoform preparation maximally by 350±20%, which is similar to receptors expressed via the LS isoform preparation (350±30%)[2]. |
| Kinase Assay | Receptors expressed via the high sensitivity (HS) isoform preparation are evaluated for Desformylflustrabromine hydrochloride modulation by coapplication of 10 μM ACh with increasing concentrations of Desformylflustrabromine hydrochloride (0.001 to 100 μM). To compare responses from different oocytes, individual responses to Desformylflustrabromine hydrochloride application are normalized to the control responses elicited using either 10 or 100 μM ACh for receptors expressed by the HS or LS isoform preparations, respectively, for both wild-type and mutated receptors. Data are collected from at least four replicate experiments using oocytes obtained from at least two different frogs[2]. |
| References |
| Molecular Formula | C16H22BrClN2 |
|---|---|
| Molecular Weight | 357.71600 |
| Exact Mass | 356.06500 |
| PSA | 27.82000 |
| LogP | 5.34880 |
| Storage condition | 2-8℃ |
| RIDADR | NONH for all modes of transport |
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