cis-Flupenthixol
cis-Flupenthixol is an orally active dopamine receptor antagonist, with a Ki value of 1.4 nM for the Dopamine D-1 receptor and 0.74 nM for the Dopamine D-2 receptor. cis-Flupenthixol blocks dopamine receptors in the medial preoptic area and striatum, impairs male mating behavior, and reduces the concentrations of striatal dopamine metabolites. cis-Flupenthixol alters striatal acetylcholine concentrations in a time-dependent manner and enhances Apomorphine (HY-12723)-induced stereotyped behaviors. cis-Flupenthixol inhibits exploratory locomotor activity and triggers a compensatory increase in dopamine turnover in the striatum and limbic regions. cis-Flupenthixol can be used in studies related to tardive dyskinesia.
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- CAS No.: 53772-82-0
- Formule: C23H25F3N2OS
- Masse moléculaire:434.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[3]|
D1 Receptor 1.4 nM (Ki) |
D2 Receptor 0.74 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Astrocyte | EC50 |
1.182 μM
Compound: 7
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Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
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[PMID: 17417631] |
In Vitro
cis-Flupenthixol potently interacts with both dopamine D1 and D2 receptors, with Ki values of 1.4 nM for D1 receptors and 0.74 nM for D2 receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
cis-Flupenthixol (20.0 μg; microinjected into the medial preoptic area of the lateral ventricle; single injection) increases sedentary behavior in male rats, but does not alter other general activity indices[1].
cis-Flupenthixol (10.0 μg; intracerebroventricular [microinjection into the medial preoptic area]; single injection) blocks the facilitatory effect of Apomorphine (HY-12723) on sexual behavior and prolongs the intermount interval, although the drug itself has no effect on ejaculation frequency[1].
cis-Flupenthixol (0.8-1.2 mg/kg/day; oral administration; continuously added to drinking water; 14 months) induces functional dopamine receptor supersensitivity in male Wistar rats, which is specifically characterized by enhanced apomorphine-induced stereotyped behaviors, increased Bmax of striatal dopamine receptors after withdrawal, doubled striatal acetylcholine levels, and decreased concentrations of striatal HVA and DOPAC[2].
cis-Flupenthixol (0.625-40 μg/side, intracerebral injection) dose-dependently suppressed spontaneous exploratory activity in the nucleus accumbens and ventromedial neostriatum with minimal drug diffusion from injection sites[3].
cis-Flupenthixol (0.05-0.8 mg/kg; i.p.) inhibits exploratory spontaneous activity and rearing behavior, while increasing dopamine turnover rate in the striatum and limbic brain regions, as evidenced by elevated levels of DOPAC and HVA[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (adult male, 300-375 g, stereotaxically implanted cannulae targeting medial preoptic area)[1]
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Dosage:20.0, 40.0 μg
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Administration:i.c.v. [MPOA microinjection]; single injection
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Result:Markedly cut overall ejaculation frequency from 2.58 in the vehicle group to 0.74 at both 20.0 μg and 40.0 μg doses.
Decreased the quantity of males displaying mounting, intromission and ejaculation behaviors of varying frequencies at 20.0 μg and 40.0 μg relative to full behavioral occurrence in all vehicle subjects.
Lowered average ejaculation frequency to 1.75 (20.0 μg) and 2.00 (40.0 μg) among males capable of ejaculation.
Prolonged the first interintromission interval to 89.64 s (20.0 μg) and 70.63 s (40.0 μg), against the vehicle value of 43.74 s.
Delayed the initial ejaculation latency to 632.12 s at 20.0 μg, compared with 397.47 s in vehicle treatment.
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Animal Model:Long-Evans (adult male, 300-375 g, stereotaxically implanted cannulae targeting medial preoptic area)[1]
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Dosage:20.0 μg
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Administration:i.c.v. [MPOA microinjection]; single injection
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Result:Increased sitting behavior and showed no changes in walking, rearing, standing, lying down, grooming, eating, or drinking behaviors.
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Animal Model:Long-Evans (adult male, 300-375 g, stereotaxically implanted cannulae targeting medial preoptic area)[1]
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Dosage:10.0 μg; 10.0 μg + 0.5 μg Apomorphine
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Administration:i.c.v. [MPOA microinjection]; single injection
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Result:Exerted no obvious change to ejaculation frequency yet prolonged the first interintromission interval from 41.69 s to 62.06 s.
Neutralized apomorphine-induced elevation in ejaculation frequency and suppressed the raised proportion of males with ≥ 2 ejaculations under combined medication.
Prolonged the first interintromission interval to 83.74 s relative to apomorphine monotherapy.
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Animal Model:Sprague-Dawley (adult male, 280-320 g)[3]
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Dosage:0.625, 1.25, 10, 20, 40 μg/side
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Administration:intracerebral; injected in 1 μl/side over 45 seconds, cannula left in place 45 seconds post-injection
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Result:Suppressed exploratory locomotion in a dose-dependent manner.
Exerted no locomotor influences at low nucleus accumbens doses (0.625, 1.25 μg/side) and tested dorsolateral neostriatum doses.
Triggered no catalepsy following injections into all detected brain regions.
Elevated ipsilateral DOPAC content locally at 30–120 min after unilateral 40 μg/side injection into ventromedial neostriatum or nucleus accumbens, without alterations in contralateral and adjacent brain tissues.
Raised regional HVA levels synchronously with DOPAC elevation while keeping dopamine concentrations stable across all measured brain areas.
Chemical Information
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CAS No. 53772-82-0
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Masse moléculaire 434.52
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Formule C23H25F3N2OS
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SMILES
OCCN(CC1)CCN1CC/C=C2C3=CC(C(F)(F)F)=CC=C3SC4=CC=CC=C4\2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Pehek EA, et al. Microinjection of cis-flupenthixol, a dopamine antagonist, into the medial preoptic area impairs sexual behavior of male rats. Brain research. 1988 Mar 08;443(1-2):70-6. [Content Brief]
[2]. Murugaiah K, et al. Increased striatal acetylcholine after 14 months cis-flupenthixol treatment in rats suggests functional supersensitivity of dopamine receptors. Life sciences. 1982 Jul 12;31(2):181-8. [Content Brief]
[3]. Ahlenius S, et al. Suppression of exploratory locomotor activity and increase in dopamine turnover following the local application of cis-flupenthixol into limbic projection areas of the rat striatum. Brain research. 1987 Jan 27;402(1):131-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
cis-Flupenthixol Related Classifications
HY-184837 Related Classifications
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