BRL 54443 maleate
BRL 54443 (MALEATE) is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.
For research use only. We do not sell to patients.
- CAS No.: 1197333-54-2
- Formula: C18H22N2O5
- Molecular Weight:346.38
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All 5-HT Receptor Isoforms
More
Biological Activity
|
5-HT1E Receptor |
Despite its low affinity for other receptors [5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT1F receptors[1].
In DG membranes, BRL54443 selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production (IC50=14 nM). BRL 54443 (MALEATE) (MALEATE) also induces contraction (-log EC50=6.52)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1197333-54-2
-
Molecular Weight 346.38
-
Formula C18H22N2O5
-
SMILES
OC1=CC2=C(NC=C2C3CCN(C)CC3)C=C1.O=C(O)/C=C\C(O)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Klein MT, et al. Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-867. [Content Brief]
[2]. McKune CM, et al. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95. [Content Brief]
[3]. Klein MT, et al. Distribution of 5-ht(1E) receptors in the mammalian brain and cerebral vasculature: an immunohistochemical and pharmacological study. Br J Pharmacol. 2012 Jun;166(4):1290-302. [Content Brief]
[4]. Granados-Soto V, et al. The role of peripheral 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F serotonergic receptors in the reduction of nociception in rats. Neuroscience. 2010 Jan 20;165(2):561-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BRL 54443 maleate Related Classifications
HY-13221A Related Classifications
Powered by Bioz