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 No.: 104639-01-2
- Formule: C18H24N2S
- Masse moléculaire:300.46
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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
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Activité biologique
Description
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; 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.
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Animal Model:Sprague-Dawley (male, 180-240 g, Cocaine·HCl-induced hyperactivity model)[1]
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Dosage:20 mg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:Sprague-Dawley (female, 200-225 g, Cocaine·HCl-induced hyperactivity model)[1]
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Dosage:20 mg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:Sprague-Dawley (male, 207-255 g, Cocaine·HCl-induced hyperactivity model)[1]
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Dosage:20 mg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:Sprague-Dawley (male, 180-240 g, saline-challenged healthy model)[1]
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Dosage:20 mg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:Sprague-Dawley (male, 207-255 g, healthy model)[1]
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Dosage:20 mg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:Sprague-Dawley (male, female, healthy model)[1]
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Dosage:20 mg/kg
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Administration:i.v.; single dose
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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
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CAS No. 104639-01-2
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Masse moléculaire 300.46
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Formule C18H24N2S
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SMILES
S=C=NC1CCN(CC1)C2(C=3C=CC=CC3)CCCCC2
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fourphit Related Classifications
HY-187585 Related Classifications
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Keywords
- Fourphit
- 104639-01-2
- Dopamine Transporter
- Calcium Channel
- dopamine transporter
- male Sprague-Dawley rats
- mouse brain neurons
- striatal tissue
- female Sprague-Dawley rats
- cocaine addiction
- nerve terminal preparations
- phencyclidine receptor
- neuronal dihydropyridine calcium channels
- cocaine abuse
- Inhibitor
- inhibitor
- inhibit