Estrogens may reduce mortality and ischemic damage caused by middle cerebral artery occlusion in the female rat.
The present study provides the first evidence that estrogens exert neuroprotective effects in an animal model of ischemia and suggests that estrogen may be a useful therapy to protect neurons against the neurodegenerative effects of stroke.
Ophthalmic drug design based on the metabolic activity of the eye: Soft drugs and chemical delivery systems
This review will concentrate on-adrenergic agonists and anti-inflammatory corticosteroids, where clinical results obtained with new chemical entities exist to support the advantages of such metabolism-focused, ophthalmic-specific drug design approaches.
Octanol-water partition: searching for predictive models.
The recently developed, molecular size-based approach is reviewed, and it is argued that introduction of three-dimensionality allows the elimination of many empirically derived fragment constants without a significant deterioration of the predictive accuracy.
Soft drugs—10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: Loteprednol etabonate
Receptor binding studies of soft anticholinergic agents
The potency as measured by the pK i values was found to be related to geometric, electronic, and lipophilicity descriptors for the soft anticholinergics containing at least 1 tropine moiety in their structure.
Brain-Targeted Drug Delivery
Site-target indexing and the use of targeting enhancement factors can be used to quantitatively assess the site-targeting effectiveness from a pharmacokinetic perspective of chemical delivery systems.
Soft glucocorticoid design: structural elements and physicochemical parameters determining receptor-binding affinity.
According to data, receptor binding affinity at the GR is dramatically increased by 6alpha- or 9alpha-halogenation and it also tends to increase with increasing lipophilicity, which accounts for a large portion of the variability in RBA.
Use of 2-Hydroxypropyl-β-cyclodextrin as a Solubilizing and Stabilizing Excipient for Protein Drugs
Data suggest that this starch derivative may be a potentially useful excipient for protein drugs intended for parenteral use and the safety of HPCD and its well-characterized chemical composition are suggested.
Improved delivery through biological membranes. XXII. Synthesis and distribution of brain-selective estrogen delivery systems
Improved delivery through biological membranes. 3. Delivery of N-methylpyridinium-2-carbaldoxime chloride through the blood-brain barrier in its dihydropyridine pro-drug form.
Administration of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, the pro-drug form of 2-PAM, resulted in an average of 13-fold increase in the amount of 2-PAM delivered into the brain of…