104639-01-2
Chemical Structure
Fourphit
- CAS No.: 104639-01-2
- Formula:C18H24N2S
- Molecular Weight:300.46
IUPAC Name: 4-isothiocyanato-1-(1-phenylcyclohexyl)piperidine
InChIKey: QAHYIAVTWZVTMY-UHFFFAOYSA-N
SMILES: S=C=NC1CCN(CC1)C2(C=3C=CC=CC3)CCCCC2
Biological Activity: 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[1][2].
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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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References
- [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.