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Binding studies using the enantiomers of the synthetic cannabinoid 7-hydroxy-delta 6-tetrahydrocannabinol 1,1-dimethylheptyl homolog in preparations of rat brain cortical membranes reveal that the (+)-(3S,4S) enantiomer HU-211 blocks N-methyl-D-aspartate (NMDA) receptors in a stereospecific manner and that the interaction occurs at binding sites distinct(More)
The non-psychotropic cannabinoid (+)-(3S,4S)-7-hydroxy-delta 6- tetrahydrocannabinol 1,1-dimethylheptyl (HU-211), a stereoselective inhibitor of the N-methyl-D-aspartate (NMDA) receptor, protects primary cultures of rat forebrain against NMDA receptor-mediated neurotoxicity. Cell mortality produced by exposure for 10 min to NMDA or glutamate was reduced to(More)
Oxygen caused a reversible inhibition (switch-off) of nitrogenase activity in whole cells of four strains of diazotrophs, the facultative anaerobe Klebsiella pneumoniae and three strains of photosynthetic bacteria (Rhodopseudomonas sphaeroides f. sp. denitrificans and Rhodopseudomonas capsulata strains AD2 and BK5). In K. pneumoniae 50% inhibition of(More)
2 After experimental status epilepticus, many dentate granule cells born into the postseizure 14 environment migrate aberrantly into the dentate hilus. Hilar ectopic granule cells (HEGCs) have 15 also been found in persons with epilepsy. These cells exhibit a high rate of spontaneous activity, 16 which may enhance seizure propagation. Electron microscopic(More)
The effects of the synthetic non-psychoactive cannabinoid (+)-(3S,4S)-7-hydroxy-delta 6-tetrahydrocannabinol 1,1-dimethylheptyl (HU-211) on the activity of the N-methyl-D-aspartate (NMDA) receptor/ion channel were examined. HU-211 non-competitively blocks the increase in binding of [3H]N-[1-(2-thienyl)-cyclohexyl]piperidine ([3H]TCP) induced by the(More)
45Ca accumulation was studied autoradiographically as a marker for lethally injured brain tissue following closed head injury (CHI), and applied to an investigation of the neuroprotective effect of the non-psychoactive cannabinoid (+)-(3S,4S)-7-hydroxy-D-6 tetrahydro-cannabinol 1,1-dimethylheptyl (HU-211). Amassment of 45Ca in rat brain was examined 24 or(More)
Binding of the labeled anticonvulsant drug [3H]dibenzocycloalkenimine [(3H]MK-801 to the N-methyl-D-aspartate (NMDA) receptor and its dissociation from the receptor at 25 degrees C are slow processes, both of which follow first order kinetics (t1/2 approximately equal to 70 and 180 min, respectively). Both reactions are markedly accelerated by glutamate and(More)
2 In temporal lobe epilepsy, loss of inhibitory neurons and circuit changes in the dentate 15 gyrus promote hyperexcitability. This hyperexcitability is compensated to the point that dentate 16 granule cells exhibit normal or even subnormal excitability under some conditions. This study 17 explored the possibility that compensation involves enhanced tonic(More)
PURPOSE Amino acid esters containing tertiary or quaternary nitrogen heterocycles were synthesized for dexanabinol (1) and evaluated as water-soluble prodrugs or congeners. METHODS Syntheses were performed by conventional methods; stability studies in water, blood (rat, dog, human) and assay-media were performed by HPLC; NMDA receptor binding was(More)