Description
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
Product information
CAS Number: 874882-92-5
Molecular Weight: 664.79
Formula: C36H48N4O8
Chemical Name: (2E)-but-2-enedioic acid; bis(1-[(propan-2-yl)amino]-3-[2-(1H-pyrrol-1-yl)phenoxy]propan-2-ol)
Smiles: CC(C)NCC(O)COC1=CC=CC=C1N1C=CC=C1.CC(C)NCC(O)COC1=CC=CC=C1N1C=CC=C1.OC(=O)/C=C/C(O)=O
InChiKey: MCHSBYUSDSJLAQ-WXXKFALUSA-N
InChi: InChI=1S/2C16H22N2O2.C4H4O4/c2*1-13(2)17-11-14(19)12-20-16-8-4-3-7-15(16)18-9-5-6-10-18;5-3(6)1-2-4(7)8/h2*3-10,13-14,17,19H,11-12H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;;2-1+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Isamoltane exhibits 27-fold selectivity for the 5-HT1B receptor over 5-HT1A (IC50=1070 nM) in rat brain membranes. Isamoltane (0.01-10 µM) increases the [3H]-overflow elicited by electrical stimulation in a concentration-dependent manner in rat cortical slices.
In Vivo:
Isamoltane (0.3-30 mg/kg; i.p) does not alter the accumulation of 5-HTP in the rat hippocampus, and increases 5-HT synthesis in cortical tissue. Isamoltane reduces 5-HTP accumulation in the striatum.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.