MedChem 2005 - Targeting the Brain, Successes and Pitfalls
25/11/2005
08:00
Registration
08:50
Introduction
09:00
Conversion of the mushroom toxin Muscimol into THIP (Gaboxadol), a novel type of hypnotic and non-opoid analgesic
Prof. Povl KROGSGAARD-LARSEN (THE DANISH UNIVERSITY OF PHARMACEUTICAL SCIENCES, Copenhagen, Denmark)
09:50
Identification and biological evaluation of high affinity TRPV1 (VR1) vanilloid receptor antagonists
Dr Nicholas CARRUTHERS (JOHNSON & JOHNSON R&D, San Diego, United States)
10:40
Coffee break & poster session
11:10
High throughput surface activity profiling in the prediction of blood-brain-barrier permeation
Prof. Paavo KINNUNEN (UNIVERSITY OF HELSINKI, Helsinki, Finland)
11:30
Towards a molecular understanding of presynaptic function: emerging targets for drug action
Dr Thomas C. SUDHOF (HOWARD HUGHES MEDICAL INSTITUTE, DALLAS, TX, United States)
12:20
Sandwich lunch & poster session
13:20
Medicinal chemistry of CB1 cannabinoid receptor antagonists
Dr Jos LANGE (ABBOTT HEALTHCARE, WEESP, The Netherlands)
14:30
Optimisation of brain penetration in drug discovery
Dr Peter EDDERSHAW (UCB SA, CAMBRIDGE, United Kingdom)
15:20
P-glycoprotein, the gatekeeper: influence on the tissue distribution of the 5-ht1a antagonist P-[ 18F]MPPF , an ex vivo study in rats
Dr Alain PLENEVAUX (LIEGE UNIVERSITY CYCLOTRON, Liege, Belgium)
15:40
Coffee break & poster session
16:10
Quantitative in vivo microdialysis study on the influence of multidrug transporters on the blood-brain barrier passage of oxcarbazepine: concomitant use of hippocampal monoamines as pharmacodynamic markers for the anticonvulsant activity.
Dr Ralph CLINCKERS (VUB, Jette - Brussel, Belgium)
16:30
Discovery of GABA-A α2/3 subtype selective agonists for the treatment of anxiety
Dr Michael RUSSELL (MERCK SHARP & DOHME, Harlow, United Kingdom)
