Author: Waarde, A.

Source: Current Pharmaceutical Design, Volume 6, Number 16, 1 November 2000 , pp. 1593-1610(18)

Publisher: Bentham Science Publishers

Abstract:

Many physiological and biochemical measurements can be performed noninvasively in humans with modern imaging techniques like magnetic resonance imaging (MRI), positron emission tomography (PET) or single-photon emission computed tomography (SPECT). This review focuses on the monitoring of drug-receptor interactions in patients and healthy volunteers with PET. Such studies depend on the availability of a suitable radioligand; they are already possible for classical and atypical neuroleptics, anxiolytics, antidepressants, anticholinergics, antihistamines, antiepileptics, beta-blockers and hypnotic drugs. In Phase I-II human studies, measurements of plasma pharmacokinetics can be combined with images of receptor occupancy and be quantitatively related to pharmacologic effects which are induced in the same subjects. Optimal dosing schedules can be defined and valuable information for the design of Phase III studies can be acquired. Moreover, the effect of interventions (e.g. change of dose, additional medication) can be predicted. Medical imaging techniques will play an increasing role in clinical pharmacology and allow well-informed go/no-go decisions in future drug development.

Keywords: Receptor Occupancy; Magnetic Resonanace Imaging; Single Photon emission computed tomography(SPECT); Receptor-rich regions; Neuroleptics; Neurotransmitter; Neuroimaging techniques; Serotonine antagonists; Muscarinc antagonist; Extrapyramidal symptoms(EPS); Antihistamines; Hypnotics; Pitfalls; Pseudo-equilibrium; Free Radioligand Concentration

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612003398951

Publication date: 2000-11-01

More about this publication?

• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

Related content

• In this: publication
• By this: publisher
• In this Subject: Pharmacology
• By this author: Waarde, A.

Website © Publishing Technology. Article copyright remains with the publisher, society or author(s) as specified within the article.

• Terms and conditions
• Privacy policy
• Information for advertisers