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Chlorpromazine HCl dopamine receptor antagonist

Catalog No.B1480
Size Price Stock Qty
10mM (in 1mL DMSO)
$80.00
In stock
Evaluation Sample
$28.00
In stock
50mg
$68.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Chlorpromazine HCl

Protocol

Cell experiment [1]:

Cell lines

Hippocampus neurons

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

10 ~ 100 μM

Applications

Chlorpromazine HCl at 10 ~ 100 μM dose-dependently decreased mIPSC amplitude. Besides, Chlorpromazine HCl significantly accelerated the decay of mIPSC at the concentrations ≥ 30 μM in a dose-dependent manner. However, there was no significant difference on the 10 ~ 90% rise time between the control group and the Chlorpromazine HCl treatment groups.

Animal experiment [2]:

Animal models

A rat model of hypoxia

Dosage form

30 mg/kg; i.p.

Applications

In a rat model of hypoxia, Chlorpromazine HCl reduced irreversible loss of synaptic transmission in brain tissues. Chlorpromazine HCl also significantly delayed the occurrence of the hypoxia-induced spreading depression in rats by slowing down the influx of Ca2+ into neurons.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Mozrzymas JW, Barberis A, Michalak K, Cherubini E. Chlorpromazine inhibits miniature GABAergic currents by reducing the binding and by increasing the unbinding rate of GABAA receptors. J Neurosci. 1999 Apr 1;19(7):2474-88.

[2]. Balestrino M, Somjen GG. Chlorpromazine protects brain tissue in hypoxia by delaying spreading depression-mediated calcium influx. Brain Res. 1986 Oct 22;385(2):219-26.

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Chemical Properties

Cas No. 69-09-0 SDF Download SDF
Chemical Name 3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine;hydrochloride
Canonical SMILES CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl.Cl
Formula C17H19ClN2S.HCl M.Wt 355.33
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Dopamine receptors are a class of G protein-coupled receptors that are prominent in the central nervous system. Dopamine receptors are implicated in many neurological processes. Thus, dopamine receptors are common neurologic drug targets. Antipsychotics are often dopamine receptor antagonists while typically psychostimulants are indirect agonists of dopamine receptors. Chlorpromazine is a dopamine antagonist.

In vitro: The antipsychotic activity of chlorpromazine has been associated with its ability to act as a dopamine-receptor antagonist. the manner in which chlorpromazine, with its phenothiazine ring structure, interacted with a receptor for dopamine. Furthermore, chlorpromazine inhibited the binding of [3H]spiperone, and the inhibition curve was consistent with a single class of binding sites [1].

In vivo: Daily administration of chlorpromazine to rats for 21 days induced catalepsy, tolerance to catalepsy and locomotor sensitization following PCP challenge. Results suggest that daily chlorpromazine treatment induced DA/NMDA-receptor sensitization to total locomotor activity following PCP challenge [2].

Clinical trial: Chlorpromazine is clinical used as a conventional antipsychotic drug that has been used for the management of psychotic disorders since its FDA approval in 1954.

Reference:
[1] Harrold MW, Chang YA, Wallace RA, Farooqui T, Wallace LJ, Uretsky N, Miller DD.  Charged analogues of chlorpromazine as dopamine antagonists. J Med Chem. 1987 Sep;30(9):1631-5.
[2] Nsimba SE.  Effects of daily chlorpromazine administration on behavioural and physiological parameters in the rat. Indian J Physiol Pharmacol. 2009 Jul-Sep;53(3):209-18.