BRL-54443
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Cat.No：IB2760 Solarbio
CAS：57477-39-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Neuronal Signal Pathway > BRL-54443
Product Information
| CAS | 57477-39-1 |
| Name | BRL-54443 |
| Molecular Formula | C14H18N2O |
| Molecular Weight | 230.31 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD01861184 |
| SMILES | CN1CCC(CC1)C2=CNC3=C2C=C(C=C3)O |
| InChIKey | WKNFADCGOAHBPG-UHFFFAOYSA-N |
| InChI | InChI=1S/C14H18N2O/c1-16-6-4-10(5-7-16)13-9-15-14-3-2-11(17)8-12(13)14/h2-3，8-10，15，17H，4-7H2，1H3 |
| PubChem CID | 2438 |
| Target Point | 5-HT Receptor |
| Passage | Neuronal Signaling；GPCR & G Protein |
| Background | BRL-54443 is a 5-HT1E and 5-HT1F receptor agonist. |
| Biological Activity | BRL 54443 是一种强效的 5-HT1E和5-HT1F受体激动剂（Ki 值分别为 1.1 nM 和 0.7 nM），对5-HT1A，5-HT1B，5-HT1D受体具有弱的结合亲和力。[1] |
| In Vitro | The tryptamine-related agonist BRL54443 [5-hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole] binds 5-HT(1E)receptors with high affinity and some selectively; it binds equally well to 5-HT(1F)receptors(K(i)≈ 1 nM).[1] The 5-HT(1E/1F)receptor agonist BRL 54443 induced contraction(-log EC(50)= 6.52).[2] In dentate gyrus(DG)membranes，BRL54443，a 5-ht(1E)/5-HT(1F)agonist，selectively stimulated 5-ht(1E)receptors and potently inhibited forskolin-dependent cAMP production(IC = 14 nM).[3] |
| In Vivo | Ipsilateral，but not contralateral，peripheral administration of the 5-HT(1)receptor agonists BRL54443(5-HT(1E/1F); 3-300 microg/paw)significantly reduced formalin-induced rats' flinching.[4] |
| Data Literature Source | [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):860-7. [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. [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. [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. |
| Unit | Bottle |
| Specification | 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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