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
Physiological aspects, Somatotropin, Structure-activity relationships (Pharmacology), Neuropeptides, Hippocampus (Brain), Spinal cord, Structure-activity relationship (Pharmacology)

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New delta-opioid antagonists as pharmacological probes

Article Abstract:

Recent research developments have shed light on possible medicinal use for the delta-receptor-selective opioid antagonists, Tyr-Tic and Dmt-Tic. Alterations on the structure of the Tyr-Tic peptide, TIPP, yielded a series of antagonists with moderate to high bioactivity. On the other hand, the dipeptide H-Tyr-Tic-NH2 exhibited a moderate delta antagonist activity in vitro. Still another research finding highlighted the creation of Dmt-Tic di-and tri-peptides through the addition of methyl groups at the 2' and 6' position of tyrosine.

author: Bryant, Sharon D., Salvadori, Severo, Cooper, Peter S., Lazarus, Lawrence H.
Opioids, Psychotropic drugs, Opioid receptors

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Time to reassess chiral aspects of beta-adrenoceptor antagonists: clinical evidence for harmful effects of the non-beta-blocking enantiomers

Article Abstract:

The beta-adrenoceptor antagonists is widely accepted as the most effective drug for the prevention of sudden cardiac death. However, a few studies reveal that the d-enantiomers present in different beta-adrenoceptor antagonists can cause harm such as antiarrhythmic class 1 effects, inhibition of the transformation thyroxin to triiodothyronin and antiarrhythmic class 3 effects. It is therefore beneficial to forego using racemic beta-adrenoceptor antagonists which contain d-enantiomers and instead use the l-enantiomers.

author: Stoschitzky, Kurt, Klein, Werner, Linder, Wolfgang
Prevention, Cardiac arrest, Enantiomers, Beta adrenoceptors, Adrenergic beta receptors

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subjects list: Research
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