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Art. -Nr.: HY-187585

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Fourphit

Fourphit is a dopamine transporter (DAT) inhibitor and phencyclidine (PCP) receptor binding agent. Fourphit irreversibly acylates the DAT [³H]methylphenidate binding site, reversibly binds to the PCP receptor, and sensitizes neuronal L-type DHP calcium channels. Fourphit attenuates K⁺-stimulated ⁴⁵Ca²⁺ uptake at high concentrations, and after its pretreatment, Nifedipine (HY-B0284) effectively inhibits this uptake without affecting resting calcium uptake. Fourphit reduces cocaine-induced hyperactivity, decreases cocaine-induced rearing frequency, enhances cocaine-induced thigmotaxis, elicits an acute increase in locomotor activity, and suppresses dark-cycle activity. Fourphit is used in research related to cocaine abuse and addiction.

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CAS. Nr.: 104639-01-2
Formel: C₁₈H₂₄N₂S
Molecular Weight:300.46

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Fourphit Chemical Structure

CAS. Nr.: 104639-01-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

In Vitro

Fourphit irreversibly inhibits the binding of Cocaine to the dopamine transporter in vitro^[1].
Fourphit (10-100 μM; 15 min) does not alter K⁺-stimulated or resting ⁴⁵Ca²⁺ uptake in isolated mouse brain neurons at low concentrations, but at high concentrations it reduces net K⁺-stimulated ⁴⁵Ca²⁺ uptake by 26%; furthermore, pretreatment with this compound produces a 33% inhibition of Nifedipine on K⁺-stimulated ⁴⁵Ca²⁺ uptake in these neurons^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Fourphit (20 mg/kg; intravenous injection; single administration) reduces locomotor activity in female and male Sprague-Dawley rats during the first 1 h after Cocaine·HCl challenge ^[1].
Fourphit (20 mg/kg; i.v.; single administration) has no significant effect on spontaneous activity in male Sprague-Dawley rats treated with saline^[1].
Fourphit (20 mg/kg; i.v.; single administration) produces a slight acute increase in locomotor activity in male Sprague-Dawley rats, but decreases dark-phase locomotor activity by 26% over an 11-h period^[1].
Fourphit (20 mg/kg; i.v.; single administration) does not reduce specific ex vivo [³H]methylphenidate binding in striatal tissue of male or female Sprague-Dawley rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (male, 180-240 g, Cocaine·HCl-induced hyperactivity model)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; single dose
Result:

Attenuated Cocaine·HCl-induced locomotor activity, with a 56% reduction in total activity, 62% reduction in ambulatory activity, and 36% reduction in nonambulatory activity during the first 40 min post-Cocaine·HCl challenge.

Animal Model:

Sprague-Dawley (female, 200-225 g, Cocaine·HCl-induced hyperactivity model)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; single dose
Result:

Reduced Cocaine·HCl-induced total activity by 27.6% (from 10,290 to 7,446 counts/h), ambulatory activity by 28.7% (from 8,217 to 5,858 counts/h), and nonambulatory activity by 23.4% (from 2,073 to 1,588 counts/h) over the 1-h post-Cocaine·HCl challenge period.

Animal Model:

Sprague-Dawley (male, 207-255 g, Cocaine·HCl-induced hyperactivity model)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; single dose
Result:

Caused a 34% reduction in total activity (from 2963 to 1963 counts) and 43% reduction in ambulatory activity (from 2233 to 1268 counts) during the 15-40 min period post-Cocaine·HCl challenge.
Exhibited 46% fewer rearings (from 381 to 205 total rearings) and 356% more thigmotactic behaviors (from 16 to 57 total cage circles) compared to controls over the 90-min post-challenge period.

Animal Model:

Sprague-Dawley (male, 180-240 g, saline-challenged healthy model)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; single dose
Result:

Had no significant effect on total, ambulatory, or nonambulatory activity in response to saline challenge; total activity counts were 442 counts/h for Fourphit-treated rats vs. 382 counts/h for vehicle-treated controls.

Animal Model:

Sprague-Dawley (male, 207-255 g, healthy model)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; single dose
Result:

Increased acute ambulatory activity (5-35 min post-injection) (170 counts/30 min vs. 56 counts/30 min for controls).
Reduced ambulatory activity during the dark cycle by 26% (from 7862 to 5856 counts/11 h) compared to controls.

Animal Model:

Sprague-Dawley (male, female, healthy model)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; single dose
Result:

Did not alter ex vivo specific [3H]methylphenidate binding in striatal tissue at 1 h (fresh tissue: 77,400 vs. 70,880 CPMs/mg protein for controls) or 26 h (frozen tissue: male cocaine-challenged: 51,400 vs. 43,200 CPMs/mg protein; female cocaine-challenged: 51,200 vs. 53,800 CPMs/mg protein; male saline-challenged: 36,900 vs. 39,900 CPMs/mg protein) post-treatment.

Chemical Information

CAS. Nr. 104639-01-2
Molecular Weight 300.46
Formel C₁₈H₂₄N₂S
SMILES

S=C=NC1CCN(CC1)C2(C=3C=CC=CC3)CCCCC2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Schweri MM, et al. Fourphit, an acylating phencyclidine derivative, attenuates cocaine-induced hyperactivity in rats. Pharmacology, biochemistry, and behavior. 1998 Jul;60(3):615-23.

[2]. Rice KC, et al. Interactions between phencyclidine and nifedipine at 45Ca2(+)-uptake sites on mouse brain neurons. Biochem Pharmacol. 1990 Jun 1;39(11):1825-7.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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