Pharmacokinetics of Deramciclane, a Novel Anxiolytic Agent, after Intravenous and Oral Administration

  title={Pharmacokinetics of Deramciclane, a Novel Anxiolytic Agent, after Intravenous and Oral Administration},
  author={Risto K. Huupponen and Outi Paija and Markku Salonen and Harry Bj{\"o}rklund and Juha Rouru and Markku I. Anttila},
  journal={Drugs in R \& D},
AbstractBackground and objective: Deramciclane is a new compound that has shown anxiolytic effects in animal experiments and in human studies. The aim of this study was to determine the pharmacokinetic parameters of deramciclane after intravenous and oral administration, and its oral bioavailability. Methods: Deramciclane 30mg was given intravenously and orally as a tablet and as solution in an open, randomised, crossover three-period trial to 12 healthy male volunteers. Oral bioavailability… 
1 Citations

Synthesis of deramciclane* labeled with tritium in various positions

[(1R)-endo]-(+)-3-bromocamphor was dehalogenated with tritium gas to [3-3H]camphor and via [3-3H]phenylborneol converted to [3-3H]deramciclane isolated as the fumarate salt (specific activity 51.8



Pharmacokinetics of deramciclane in dogs after single oral and intravenous dosing and multiple oral dosing

It is suggested that the metabolic capacity was not sufficient to eliminate deramciclane in a linear manner with increasing dose as the AUC0–∞ increased disproportionally to the dose after both intravenous and oral dosing.

Pharmacokinetics and safety of deramciclane during multiple oral dosing.

The pharmacokinetics of deramciclane is linear over the dose range of 10 - 60 mg at steady-state and the slight non-linearity within the dose levels during repeated administration of seven days was regarded as clinically irrelevant.

The single dose pharmacokinetics and safety of deramciclane in healthy male volunteers

The pharmacokinetics and tolerability of a new putative non‐benzodiazepine type anxiolytic compound deramciclane was studied in two consecutive studies and was safe, and was well tolerated at each dose level.

Pharmacokinetics of Deramciclane in Dogs

Plasma levels of deramciclane were determined by a highly sensitive, validated gas chromatograpic-nitrogen selective detection (GC-NPD) method using a solid-phase extraction (SPE) technique and suggested a tendency toward non-linear pharmacokinetics.

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

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.

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,

Goodman & Gilman's The Pharmacological Basis of Therapeutics

Goodman and Gilman's the pharmacological basis of therapeutics , Goodman and Gilmann's the pharmaceutica basis for drug discovery, and more.