Zacopride HCl is a highly efficient 5-HT3 receptor antagonist, with Kis values of 5-HT3 and 5-HT4 receptors of 0.38 and 373 nM respectively. Zacopride HCl is also a moderate IK1 channel agonist. Zacopride HCl has significant antiarrhythmic and cardioprotective effects.

Physicochemical Properties

Molecular Formula	C15H21CL2N3O2
Molecular Weight	346.25
Exact Mass	345.101
CAS #	101303-98-4
PubChem CID	9928181
Appearance	White to off-white solid powder
Melting Point	158-160 °C
LogP	3.65
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	22
Complexity	387
Defined Atom Stereocenter Count	0
InChi Key	ITXVOUSORXSTQH-UHFFFAOYSA-N
InChi Code	InChI=1S/C15H20ClN3O2.ClH/c1-21-14-7-12(17)11(16)6-10(14)15(20)18-13-8-19-4-2-9(13)3-5-19;/h6-7,9,13H,2-5,8,17H2,1H3,(H,18,20);1H
Chemical Name	4-amino-N-(1-azabicyclo[2.2.2]octan-3-yl)-5-chloro-2-methoxybenzamide;hydrochloride
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

References

[1]. Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor. Pharmacol Res. 1999;39(5):375-382. [2]. Zacopride: anxiolytic profile in rodent and primate models of anxiety. J Pharm Pharmacol. 1988;40(4):302-305. [3]. Zacopride in schizophrenia: a single-blind serotonin type 3 antagonist trial. Arch Gen Psychiatry. 1992;49(9):751-752.

Additional Infomation

See also: Zacopride Hydrochloride (annotation moved to).

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (288.81 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (7.22 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.8881 mL	14.4404 mL	28.8809 mL
	5 mM	0.5776 mL	2.8881 mL	5.7762 mL
	10 mM	0.2888 mL	1.4440 mL	2.8881 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.