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5-Carboxamidotryptamine maleate (5-CT maleate) 74885-72-6

5-Carboxamidotryptamine maleate (5-CT maleate) 74885-72-6

CAS No.: 74885-72-6

5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 receptor agonist (act
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5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 receptor agonist (activator).

Physicochemical Properties


Molecular Formula C15H17N3O5
Molecular Weight 319.312583684921
CAS # 74885-72-6
Related CAS # 5-Carboxamidotryptamine;74885-09-9
Appearance Solid powder
SMILES

C(/C(=O)O)=C/C(=O)O.C(C1=CNC2C=CC(C(=O)N)=CC1=2)CN

HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets 5-HT1A Receptor 5-HT1B Receptor 5-HT1D Receptor 5-HT5 Receptor 5-HT7 Receptor
ln Vitro [3H] 5-Carboxamidotryptamine (5-CT) has low non-specific binding and high affinity (Kd = 0.38 nM) for 5-HT1D sites in the bovine substantia nigra. Its binding is also fast, reversible, and saturable[2]. [3H]-5-Carboxamidotryptamine (5-CT) tagged a similar number of binding sites (403 and 362 fmol/mg protein, respectively) in the bovine substantia nigra, and binding is guanine nucleotide-sensitive[2].
ln Vivo In anesthetized Wistar rats (serotonin depletion and treated with 20 mg/kg corticosterone), topical 5-carboxamidotryptamine (0.01-1000 μM) to the exposed dura mater encephala causes decreases in diastolic blood pressure, variable changes in meningeal blood flow, and increases in conductance (i.e. dilatation) in the middle meningeal artery[1].
References

[1]. 5-HT7 receptor-mediated meningeal dilatation induced by 5-carboxamidotryptamine in rats is not altered by 5-HT depletion and chronic corticosterone treatment. Proc West Pharmacol Soc. 2011;54:57-61.

[2]. [3H]-5-carboxamidotryptamine labels 5-HT1D binding sites in bovine substantia nigra. Br J Pharmacol. 1993 Aug;109(4):1206-11.

[3]. Effects of the non-selective 5-HT receptor agonist, 5-carboxamidotryptamine, on plasma glucose levels in rats. Eur J Pharmacol. 1998 Oct 16;359(1):81-6.


Solubility Data


Solubility (In Vitro) DMSO: 50 mg/mL (156.59 mM)
H2O: 25 mg/mL (78.29 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1318 mL 15.6588 mL 31.3175 mL
5 mM 0.6264 mL 3.1318 mL 6.2635 mL
10 mM 0.3132 mL 1.5659 mL 3.1318 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.