Drug Development Research
February 1, 2007
Abstract Microdosing of experimental therapeutics in humans offers a number of benefits to the drug development process. Microdosing, conducted under an exploratory Investigational New Drug (IND) application, entails administration of a sub‐pharmacological dose of a new chemical entity (NCE) that allows for early evaluation of human pharmacokinetics. Such information can be pivotal for: (1)...
Drug Development Research
September 1, 1994
Charles W. Bradberry
14 citations
Abstract This overview summarizes the results of microdialysis studies into the effects of several psychoactive drugs on extracellular serotonin (5‐HT) levels in rat brain. The effects of (+)3,4‐methylenedioxymethamphetamine (MDMA, ecstasy) were examined in the brain slice preparation for comparison with parallel electrophysiological studies of the impact of (+)‐MDMA on dorsal raphe 5‐HT...
Drug Development Research
December 1, 1993
Paul C. Moser
AbstractPrevious work shows that benzodiazepines potentiate head‐twitches induced by 5‐HT agonists and that this action is not mediated via the GABA receptor complex. In the present study the involvement of adenosinergic mechanisms in this effect has been examined, as in addition to their actions at the GABA receptor, benzodiazepines also inhibit adenosine uptake. The adenosine antagonists...
Drug Development Research
1988
F. Awouters, C. J. E. Niemegeers, Anton A. H. P. Megens et al.
139 citations
Abstract Ritanserin, a novel methylenepiperidine derivative, was studied in a wide range of common pharmacological tests mainly in rats. The lowest ED 50 , 0.0070 mg/kg, was obtained against tryptamine‐induced cyanosis. At 0.037 mg/kg, tryptamine‐induced bilateral clonic seizures were inhibited. Slightly higher doses, up to 0.11 mg/kg, inhibited mescaline and 5‐hydroxytryptophan (5‐HTP)‐induced...
Drug Development Research
1983
C. J. E. Niemegeers, Françis C. Colpaert, J.e. Leysen et al.
58 citations
Abstract An intravenous dose of 20.0 mg/kg of mescaline induced a reproducible head‐twitch response in rats. Drugs with very different pharmacological activities were tested for potential inhibition of this response. Among these drugs were a large number of serotonin antagonists, including several members of the recently described selective S 2 antagonists of which ketanserin (a potent vascular...