51529-01-2 Usage
Description
Flupenthixol dihydrochloride, also known as cis-(Z)-Flupenthixol dihydrochloride, is a thioxanthene drug that functions as an antipsychotic and neuroleptic agent. It is an off-white solid and acts as a dopamine receptor antagonist, specifically targeting the dopamine D1 receptor (DRD1), which is expressed on lung alveolar type I cells and coded by the D1R gene located on human chromosome 5q35.2.
Uses
Used in Pharmaceutical Industry:
Flupenthixol dihydrochloride is used as an antipsychotic agent for the treatment of various psychiatric disorders, such as schizophrenia and bipolar disorder. It helps in managing symptoms like hallucinations, delusions, and agitation by blocking the dopamine D1 receptors in the brain.
Used in Research Applications:
Flupenthixol dihydrochloride is used as a research tool to determine the causal involvement of extracellular LS-DA (local serotonin) and LS-NE (local norepinephrine) release patterns on social play behavior. This helps in understanding the neurochemical basis of social interactions and the role of dopamine receptor D1 in these processes.
Used in Drug Infusion:
Flupenthixol dihydrochloride is also used in drug infusions, where it can be administered to patients for the management of severe psychiatric symptoms that are unresponsive to other treatments. The infusion allows for a controlled release of the drug, providing a more targeted and effective treatment option.
Biological Activity
ki: 0.38 nm for dopamine d2 receptorscis-flupenthixol is an antagonist at dopamine d2 receptors.dopamine receptor d2 is encoded by the drd2 gene. it has been suggested that dopamine receptors are the action site of antipsychotic drugs. the dopamine d2 receptor is also the main receptor for all antipsychotic drugs.
Biochem/physiol Actions
Antipsychotic; neuroleptic agent; dopamine receptor antagonist. cis-(Z)-Flupenthixol dihydrochloride?(FLU) is used to treat schizophrenia and anxiolytic and depressive disorders Dopamine D1?plays a major role in lung fluid homeostasis. It controls the airway smooth muscle tone by producing adenylyl cyclase/cAMP, that would favor airway relaxation in asthmatics. Dopamine in the lung, serves as a neurotransmitter and noradrenaline precursor.
in vitro
the effects of striatal kainic acid lesions on [3h] cis-flupenthixol and [3h]spiperone binding to dopamine receptors were examined in a previous study. significant reductions in both binding parameters were observed, and [3h] cis-flupenthixol binding was depleted to a greater level than [3h]spiperone binding. reductions in both binding were correlated with reductions in glutamic acid decarboxylase activity [1].
in vivo
in a previous animal study rats were conditioned to associate an environment with immediate or delayed effects of pre-treatment with either cis-flupenthixol or saline vehicle. results showed that vehicle-treated control animals developed the normal pattern of cpps and cis-flupenthixol-caused da receptor antagonism could prevent the expression of cocaine cpps but it did not alter the expression of cocaine-induced cpas [2].
references
[1] cross aj, waddington jl. kainic acid lesions dissociate [3h] spiperone and [3h]cis-flupenthixol binding sites in rat striatum. eur j pharmacol. 1981 may 8;71(2-3):327-32.[2] wenzel jm, su zi, shelton k, dominguez hm, von furstenberg va, ettenberg a. the dopamine antagonist cis-flupenthixol blocks the expression of the conditioned positive but not the negative effects of cocaine in rats. pharmacol biochem behav. 2013 dec;114-115:90-6. [3] cookson ib. the effects of a 50% reduction of cis(z)-flupenthixol decanoate in chronic schizophrenic patients maintained on a high dose regime. int clin psychopharmacol. 1987 apr;2(2):141-9.
Check Digit Verification of cas no
The CAS Registry Mumber 51529-01-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,1,5,2 and 9 respectively; the second part has 2 digits, 0 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 51529-01:
(7*5)+(6*1)+(5*5)+(4*2)+(3*9)+(2*0)+(1*1)=102
102 % 10 = 2
So 51529-01-2 is a valid CAS Registry Number.
InChI:InChI=1/C23H25F3N2OS.2ClH/c24-23(25,26)17-7-8-22-20(16-17)18(19-4-1-2-6-21(19)30-22)5-3-9-27-10-12-28(13-11-27)14-15-29;;/h1-2,4-8,16,29H,3,9-15H2;2*1H/b18-5+;;
