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.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1998
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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.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1997
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