Galanin and galanin antagonists: molecular and biochemical perspectives

Article Abstract:

Galanin neuropeptides affect the endocrine, central nervous and peripheral nervous systems in different mammalian species causing the inhibition of glucose-mediated insulin release and hippocampal acetylcholine release. However, galanins facilitate the release of growth hormones in the neuroendocrine system. Moreover, the galanin receptor recognition mechanism requires the presence of the galanin 1-16 N-terminal portion which functions as a galanin receptor agonist in various processes. In addition, several synthetically prepared chimeric peptides, which exhibit different therapeutic usage, have been found to function as galanin receptor antagonists.

author: Bartfai, Tamas, Fisone, Gilberto, Langel, Ulo
Somatotropin, Neuropeptides, Hippocampus (Brain), Spinal cord

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Designing therapeutically effective 5-lipoxygenase inhibitors

Article Abstract:

The three main classes of 5-lipoxygenase inhibitors can be therapeutically used in preventing allergic and inflammatory disorders associated with leukotriene synthesis. These inhibitors are classified as either redox, iron ligand or non-redox inhibitors depending on their precise mechanism of inhibition. Non-redox inhibitors such as ICID2138 and REV5901 promote enantiospecific interactions with the enzyme resulting in high levels of drug potency and selectivity. This mechanism has proven to be more effective than those taken by both redox and iron ligand inhibitors.

author: McMillan, R.M., Walker, E.R.H.
Cover Story, Arachidonic acid, Leukotrienes, Zileuton (Medication)

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Pharmacological effects of drug conjugates: is morphine 6-glucuronide an exception?

Article Abstract:

The 6- and 3-glucuronide conjugates of morphine exhibit stronger pharmacological activity than natural morphine. Similarly, sulfate conjugates have been found to feature higher pharmacological activity than their unconjugated forms. The potency of these drugs is in contrast to the pharmacological effect that usually occurs in drug conjugates. It seems that certain factors such as receptor-drug interactions and chemical solubility affect drug conjugation processes and development with regards to the drug's chemical structure and pharmacological activity.

author: Mulder, Gerard J.
Morphine

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subjects list: Physiological aspects, Structure-activity relationships (Pharmacology), Structure-activity relationship (Pharmacology), Drugs
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