Blood-brain barrier crossing

G., Folkers, G., Chretien, J. R., Raevsky, 0. A. Estimation of blood-brain barrier crossing of drugs using molecular size and shape, and H-bonding descriptors. f Drug Target. 1998, 2,151-165. 

I. Blood-Brain Barrier Crossing Nerve Growth Factor Stimulators... 

I. BLOOD-BRAIN BARRIER CROSSING NERVE GROWTH FACTOR STIMULATORS489... 

Michelot, J. Moreau, M.F. Veyre, A. Labarre, P. Me3oiiel, G. Adiphenine plasma levels and blood-brain barrier crossing in the rat. Eur.J.Drug Metab.Pharmcwokinet, 1985, 10, 273-278... 

Concerning the distribution of a drug, models have been published for log BB blood/brain partition coefficient) for CNS-active drugs (CNS, central nervous system) crossing the blood-brain barrier (BBB) [38-45] and binding to human serum albumin (HSA) [46]. 

Certain neutral technetium complexes can be used to image cerebral perfusion (Fig. 4). Those in Figure 4a and 4b have been approved for clinical use. Two other complexes (Fig. 4c and 4d) were tested in early clinical trials, but were not developed further. An effective cerebral perfusion agent must first cross the blood brain barrier and then be retained for the period necessary for image acquisition. Tc-bicisate is retained owing to a stereospecific hydrolysis in brain tissue of one of the ester groups to form the anionic complex TcO(ECD) , which does not cross the barrier. This mechanism of retention is termed metaboHc trapping. 

Toxic effects of propranolol are related to its blocking P-adrenoceptor blocking actions. They include cardiac failure, hypotension, hypoglycemia, and bronchospasm. Propranolol is lipophilic and crosses the blood—brain barrier. Complaints of fatigue, lethargy, mental depression, nightmares, hallucinations, and insomnia have been reported. GI side effects include nausea, vomiting, diarrhea, and constipation (1,2). 

A number of quaternary amines are effective at modulating nerve transmissions. They often have the disadvantage of being relatively nonselective and so possess numerous sideeffects. This contrasts with the advantage that they do not cross the blood-brain barrier and so have no central sideeffects. Clo-... 

The sedation side effect commonly observed on administration of classical antihistaminic drugs has been attributed in part to the ease with which many of these compounds cross the blood brain barrier. There have been developed recently a series of agoits, for example, terfenadine (198), which cause reduced sedation by virtue of decreased penetration into the CNS. This is achieved by making them more hydrophilic. Synthesis of a related compound, ebastine (197),... 

Temozolomide crosses the blood brain barrier and can be used for the treatment of brain tumors (e.g., glioblastoma multiforme). The most common side effects are nausea and vomiting. 

Local anaesthetics are more consistently effective than other therapies, but their use is controversial. High concentrations are needed for therapeutic benefit, but this also increases the amount crossing the blood brain barrier and entering the brain producing unwanted effects. Topical administration to the airways can reduce this. 

Dopaminergic neurotoxin that causes parkinsonism via lesion of nigrostriatal dopamine neurons in rat, mice, monkeys. Unlike the dopaminergic neurotoxin MPTP (N-methy 1-4-phenyl-1,2,3,6-tetrahydropyridine) it does not cross the blood-brain barrier. 

NT69L N Me-Arg-Lys-Pro-L-neo-Trp-f-Leu-Leu-OH Potent NT analog that crosses the blood-brain barrier Antipsychotic analgesic anorectic... 

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