5-Hydroxytryptamine-like properties of <i>m</i>-chlorophenylpiperazine: comparison with quipazine

Rokosz-Pelc, A; Antkiewicz-Michaluk, L; Vetulani, Jerzy

doi:10.1111/j.2042-7158.1980.tb12896.x

Cited by 49 publications

(10 citation statements)

References 9 publications

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“…In an attempt to explore further the sites responsible for the inhibition of DA synthesis observed with systemically administered 5-HT agonists (Rokosz-Pelc et al, 1980) we injected 5-HT into the substantia nigra. pars compacta, an area where an inhibitory effect of 5-HT on the DA nigro-striatal system has been shown (Dray et al, 1976).…”

Section: Discussionmentioning

confidence: 99%

“…It has recently been reported that rn-chlorophenylpiperazine (CPP), a potent 5-hydroxytryptamine (5-HT. serotonin) agonist (Samanin et al, 1979), reduces the synthesis of 3,4-dihydroxyphenylethylamine (DA, dopamine) in the rat striatum by a mechanism that seems to involve stimulation of 5-HT receptors (Rokosz-Pelc et al, 1980). A reduction in the synthesis of striatal DA has also been found after intracerebroventricular injection of 5-HT in rats (Awazi and Guldberg, 1978).…”

mentioning

confidence: 99%

See 1 more Smart Citation

Serotonin Agonists Reduce Dopamine Synthesis in the Striatum Only when the Impulse Flow of Nigro‐Striatal Neurons Is Intact

Spampinato

Esposito

Samanin

1985

Journal of Neurochemistry

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The effects of 5-methoxy-N, N-dimethyltryptamine (5-MeO-DMT) and m-chlorophenylpiperazine (CPP), two 5-hydroxytryptamine (5-HT, serotonin) agonists, on the accumulation of 3,4-dihydroxyphenylalanine (DOPA] were studied in the striatum of rats treated with gamma-butyrolactone (GBL). Unlike 2 mg/kg i.p. apomorphine, neither 5 mg/kg i.p. 5-MeO-DMT nor 2.5 mg/kg i.p. CPP significantly reduced the GBL-induced increase in DOPA accumulation in the striatum. 5-MeO-DMT and CPP significantly reduced DOPA accumulation in animals that had received the aromatic amino acid decarboxylase inhibitor Ro 4-4602 but not GBL. 5-HT (10 micrograms in 0.5 microliter) injected in the substantia nigra, pars compacta, like GBL, significantly increased Ro 4-4602-induced accumulation of DOPA in the striatum. The data indicate that 5-HT agonists can reduce 3,4-dihydroxyphenylethylamine (DA, dopamine) synthesis in the striatum of rats only when the impulse flow of DA neurons is intact. An indirect effect through mechanisms controlling DA synthesis in the striatum, for instance cholinergic and GABA-ergic neurons, is suggested.

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Serotonin Agonists Reduce Dopamine Synthesis in the Striatum Only when the Impulse Flow of Nigro‐Striatal Neurons Is Intact

Spampinato

Esposito

Samanin

1985

Journal of Neurochemistry

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“…3) and m-CPP (0.2 mg/kg) (Fig. 4), which has been recently described as a very potent central 5-HT agonist having a direct mode of action in the central nervous system (Maj et al, 1979 b;Rokosz-Pelc et al, 1980). The following experiments were designed to show if the antagonistic effect of Ro 11-2465 on the stimulatory action of 5-HT agonists is specific, in the sense, that it does not result from the action on the NA-ergic system, and that the antagonistic effect is not related to the inhibitory action on the uptake of 5-HT.…”

Section: Resultsmentioning

confidence: 99%

Is Ro 11-2465 (Cyan-imipramine) an antagonist of postsynaptic serotonin receptors?

Pawłowski

Kwiatek

Górka

1981

J. Neural Transmission

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Ro 11-2465, a selective inhibitor of serotonin uptake of the imipramine group, was examined for its central and peripheral antiserotonin activity. Ro 11-2465 (10 mg/kg) antagonized the stimulation of the hind limb flexor reflex in the spinal rat evoked by serotonin agonists of direct mode of action (LSD, quipazine, m-chlorophenylpiperazine). However, in doses up to 20 mg/kg it did not inhibit the clonidine-induced stimulation of the flexor reflex. It also reduced the number of the quipazine-induced head twitches in rats (ID50 = 20.1 mg/kg) and, in doses 0.3--10.0 mg/kg, dose-dependently attenuated the pressor response to serotonin in the pithed rat. Like doxepine, amitriptyline, clomipramine and imipramine, Ro 11-2465 reduced the serotonin-induced contractions of the rat stomach fundus strip (its IC50 = 5 x 10(-5) M). The obtained results indicate that like other tricyclic inhibitors of serotonin uptake, Ro 11-2465 may also weakly block the postsynaptic serotonin receptors. Additional studies with fluoxetine and Org 6582 indicate that anti-serotonin properties of tricyclic compounds are not related to the serotonin uptake blocking properties.

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“…I-Aryl-piperazine formation is now known to be a common metabolic process for drugs with the arylpiperazine moiety in the side-chain of their molecule (Caccia et al 1984). These metabolites are biologically active (Fuller et al 1980, 198la;Maj & Lewandowska 1980;Rokosz-Pelc et al 1980) and their formation may therefore be a pharmacologically significant pathway for drugs undergoing extensive cleavage of the arylpiperazine side-chain (Cervo et al 1981;Caccia et al 1982Caccia et al , 1983Fong et a1 1982).…”

mentioning

confidence: 99%

In-vivo metabolism in the rat and mouse of antrafenine to 1- m-trifluoromethylphenylpiperazine

Caccia

Conti

Notarnicola

1985

Journal of Pharmacy and Pharmacology

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The analgesic antrafenine forms 1-m-trifluoromethylphenylpiperazine (mCF3PP) during its biotransformation in the rat and mouse. At least 14 and 3% of an antrafenine dose (25 mg kg-1 p.o.) reaches the systemic circulation as mCF3PP in the mouse and rat respectively. The metabolite easily enters the brain, reaching concentrations several times those in body fluids. This, together with the fact that mCF3PP is known to produce several pharmacological effects compatible with a stimulatory action on 5-hydroxytryptamine postsynaptic receptors, suggests that this metabolite may contribute to the parent drug's pharmacological effects.

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5-Hydroxytryptamine-like properties of m-chlorophenylpiperazine: comparison with quipazine

Cited by 49 publications

References 9 publications

Serotonin Agonists Reduce Dopamine Synthesis in the Striatum Only when the Impulse Flow of Nigro‐Striatal Neurons Is Intact

Serotonin Agonists Reduce Dopamine Synthesis in the Striatum Only when the Impulse Flow of Nigro‐Striatal Neurons Is Intact

Is Ro 11-2465 (Cyan-imipramine) an antagonist of postsynaptic serotonin receptors?

In-vivo metabolism in the rat and mouse of antrafenine to 1- m-trifluoromethylphenylpiperazine

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