Studies of 1-(m-chlorophenyl)-piperazine (m-CPP), 1-(p-chlorophenyl)-piperazine (p-CPP) and 1-phenylpiperazine (PP) were carried out on rats, mice and rabbits in order to assess their stimulatory effect on the central serotonin system. It was found out that m-CPP and p-CPP evoked a characteristic syndrome in the mouse behavior. All the phenylpiperazine derivatives stimulated the flexor reflex in the spinal rat and evoked hyperthermia in rats at a high ambient temperature (28 degrees C) and in rabbits. The above effects were abolished by cyproheptadine, a drug blocking the serotonin receptors. The obtained results indicate that the phenylpiperazine derivatives studied have a central serotoninmimetic action.
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Behav Brain Res
January 2015
Max Delbrueck Center for Molecular Medicine, 13125 Berlin, Germany. Electronic address:
Serotonin is probably best known for its role in conveying a sense of contentedness and happiness. It is one of the most unique and pharmacologically complex monoamines in both the peripheral and central nervous system (CNS). Serotonin has become in focus of interest for the treatment of depression with multiple serotonin-mimetic and modulators of adult neurogenesis used clinically.
View Article and Find Full Text PDFEur J Pharmacol
March 1987
The induction of penile erections by a variety of compounds with a direct or indirect effect on serotonin (5HT) receptors was investigated in rats. L-5-Hydroxy-tryptophan (L-5HTP) induced penile erections when co-administered with nialamide and the peripheral decarboxylase inhibitor benserazide, indicating that the site of action for inducing penile erections is within the central nervous system. Penile erections were also induced by the 5HT uptake inhibitors zimelidine, fluoxetine, citalopram, Org 6997, by the 5HT-releasing agent fenfluramine and by the putative 5-HT1B receptor agonist 1-(3'-chlorophenyl)-piperazine (mCPP).
View Article and Find Full Text PDFRegioselective syntheses of substituted 2-chloroquinoxalines and derived 2-(1-piperazinyl)quinoxalines are described. Selectivity in regards to serotonin reuptake blocking and serotoninmimetic activities of the piperazinylquinoxalines is reported. In general, introduction of a 6-substituent into the piperazinylquinoxaline enhanced serotonin reuptake blocking activity and diminished serotoninmimetic activity.
View Article and Find Full Text PDFStudies of 1-(m-chlorophenyl)-piperazine (m-CPP), 1-(p-chlorophenyl)-piperazine (p-CPP) and 1-phenylpiperazine (PP) were carried out on rats, mice and rabbits in order to assess their stimulatory effect on the central serotonin system. It was found out that m-CPP and p-CPP evoked a characteristic syndrome in the mouse behavior. All the phenylpiperazine derivatives stimulated the flexor reflex in the spinal rat and evoked hyperthermia in rats at a high ambient temperature (28 degrees C) and in rabbits.
View Article and Find Full Text PDFA series of 2-(1-piperazinyl)pyrazines was synthesized and evaluated for central serotonin-like activity. The most interesting member of the series, 6-chloro-2(1-piperazinyl)pyrazine (3a), had pharmacological properties characteristic of potent central serotoninmimetic activity and only weak peripheral serotoninmimetic action. Structural similarities between 3a and serotonin are discussed.
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