Oral, Intraperitoneal and Intravenous Pharmacokinetics of Deramciclane and its N‐desmethyl Metabolite in the Rat

@article{Nemes2000OralIA,
  title={Oral, Intraperitoneal and Intravenous Pharmacokinetics of Deramciclane and its N‐desmethyl Metabolite in the Rat},
  author={Katalin Balogh Nemes and Miklos Abermann and Erzs{\'e}bet Bojti and Gy. Gr{\'e}zal and Samar al-Behaisi and Imre Klebovich},
  journal={Journal of Pharmacy and Pharmacology},
  year={2000},
  volume={52}
}
The pharmacokinetic properties of deramciclane fumarate (EGIS‐3886), a new potential anxiolitic agent, and its N‐desmethyl metabolite have been investigated in Wistar rats after 10 mg kg−1 deramciclane fumarate was administered orally, intraperitoneally or intravenously. 

Studies of the side chain cleavage of deramciclane in rats with radiolabelled compounds.

Influence of food on the oral bioavailability of deramciclane from film-coated tablet in healthy male volunteers.

  • S. DrabantK. Nemes I. Klebovich
  • Medicine
    European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
  • 2004

Comparison of the effects of deramciclane, ritanserin and buspirone on extracellular dopamine and its metabolites in striatum and nucleus accumbens of freely moving rats.

TLDR
There is at least a 5-fold margin between the anxiolytic and neuroleptic doses of deramciclane in the rat, particularly in mesolimbic regions.

BIOTRANSFORMATION OF DERAMCICLANE IN PRIMARY HEPATOCYTES OF RAT, MOUSE, RABBIT, DOG, AND HUMAN

TLDR
It was concluded that phase I metabolism in human liver cells seemed to be similar to the metabolism in the hepatocytes isolated from rat, and the rat model may be considered to be predictive for human metabolism of deramciclane.

Intraperitoneal Route of Drug Administration: Should it Be Used in Experimental Animal Studies?

TLDR
It is concluded that IP administration of drugs in experimental studies involving rodents is a justifiable route for pharmacological and proof-of-concept studies where the goal is to evaluate the effect(s) of target engagement rather than properties of a drug formulation and/or its pharmacokinetics for clinical translation.

In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers.

  • S. al-BehaisiI. Antal I. Klebovich
  • Medicine, Biology
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2002

References

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Receptor binding profile and anxiolytic‐type activity of deramciclane (EGIS‐3886) in animal models

The present series of experiments was done to characterize the properties of deramciclane, a new antiserotonergic drug, in both receptor binding studies in vitro and in a number of anxiolytic,

Comparative pharmacokinetics of deramciclane in rat, dog, rabbit and man after the administration of a single oral dose of 3 mg kg-1

TLDR
The comparative pharmacokinetic study of deramciclane indicated an intensive biotransformation in all species although the rate of biotranformation appeared to be species-dependent.

Plasma Protein Binding of Deramciclane in Different Species

TLDR
The high affinity and saturable binding of deramciclane to an acute phase component of the human plasma (AAG) necessitates careful dosage during therapeutic application and may be inhibited by several ligands known to associate with this protein.

Absorption of the new anxiolytic compound deramciclane in rats, dogs and rabbits.

TLDR
The absorption of deramciclane fumarate, a new anxiolytic compound, was studied in rats, dogs and rabbits by using 3H-camphor- or 14C-phenyl-labelled radioisomers of the substance and the substance was readily absorbed from the intestinal tract after oral administration.

Whole‐body Autoradiography and Quantitative Organ‐level Distribution Study of Deramciclane in Rats

The distribution of 3H‐labelled deramciclane (EGIS‐3886), a new 5‐HT2 antagonist with anxiolytic activity, has been investigated by whole‐body autoradiography and quantitative organ‐level

Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation

TLDR
Data indicate that deramciclane is a 5- HT2C receptor inverse agonist and occupies 5-HT2C receptors during treatment, and that chronic treatment with deramCiclane does not lead to5-HT 2C receptor down-regulation.

Comparative studies on in vitro metabolism of deramciclane in rat, dog and human liver microsomes

  • European Workshop on Drug Metabolism
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A high sensitive optimized GC-NPD method using pressure program for the determination of deramciclane and its N-desmethyl metabolite in rat plasma

  • Balaton Conference on High Performance Separation Techniques,
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Absorption and pharmacokinetics of deramciclane in rat

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