Document Detail

Cannabinoid penetration into mouse brain as determined by ex vivo binding.
MedLine Citation:
PMID:  10422786     Owner:  NLM     Status:  MEDLINE    
We have used an ex vivo binding assay in the mouse to evaluate the brain penetration of cannabinoid receptor ligands. After intraperitoneal or oral administration, the pharmacological activity linked to the compound was assessed by using by [3H]WIN 55212-2 binding on cerebellar membranes. The brain penetration was high for compounds like methanandamide or delta9-tetrahydrocannabinol but poor for synthetic agonists such as (cis)-3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-(trans)-4-(3-hydr oxypropyl)cyclohexanol (CP 55940) or, R-(+)-(2,3-dihydro-5-methyl-3-[(4-morpholinyl)methyl]pyrol[1,2,3-d e]-1,4-benzoxazin-6-yl)(1-napthalenyl)methanone monomethane-sulfonate (WIN 55212-2). After oral administration the duration of action of delta9-tetrahydrocannabinol, methanandamide and WIN 55212-2 is limited and decreased 4 h after administration. The cannabinoid CB1 receptor antagonist: N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-met hyl-1 H-pyrazole-3-carboxamide hydrochloride (SR141716A) exhibited a good brain penetration and a long duration of action.
F Petitet; B Jeantaud; P Bertrand; A Imperato
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  374     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1999 Jun 
Date Detail:
Created Date:  1999-09-13     Completed Date:  1999-09-13     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  417-21     Citation Subset:  IM    
Neurochemistry Department, CRVA, Rhône-Poulenc Rorer, Vitry-sur-Seine, France.
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MeSH Terms
Arachidonic Acids / pharmacokinetics
Binding, Competitive / drug effects
Brain / drug effects,  metabolism*
Cannabinoids / metabolism*,  pharmacokinetics
Cyclohexanols / pharmacokinetics
Morpholines / metabolism,  pharmacokinetics
Naphthalenes / metabolism,  pharmacokinetics
Piperidines / pharmacokinetics
Pyrazoles / pharmacokinetics
Radioligand Assay
Receptors, Drug / agonists,  antagonists & inhibitors
Tritium / diagnostic use
Reg. No./Substance:
0/Arachidonic Acids; 0/Benzoxazines; 0/Cannabinoids; 0/Cyclohexanols; 0/Morpholines; 0/Naphthalenes; 0/Piperidines; 0/Pyrazoles; 0/Receptors, Drug; 10028-17-8/Tritium; 134959-51-6/Win 55212-2; 150314-39-9/methanandamide; 158681-13-1/rimonabant; 83003-12-7/3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-4-(3-hydroxypropyl)cyclohexanol

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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