scholarly journals Comparison of electropharmacological effects between terfenadine and its active derivative fexofenadine using a cross-over study in halothane-anesthetized dogs to analyze variability of pharmacodynamic and pharmacokinetic profiles of terfenadine and torsadogenic risk of fexofenadine

2018 ◽  
Vol 43 (3) ◽  
pp. 183-192 ◽  
Author(s):  
Kentaro Ando ◽  
Yuji Nakamura ◽  
Mihoko Hagiwara-Nagasawa ◽  
Hiroyuki Harada ◽  
Hiroyoshi Miyamoto ◽  
...  
Keyword(s):  
Active Derivative ◽  
Pharmacokinetic Profiles ◽  
Anesthetized Dogs

Naldemedine: Peripherally Acting Opioid Receptor Antagonist for Treating Opioid-induced Adverse Effects

2020 ◽  
Vol 20 (31) ◽  
pp. 2830-2842
Author(s):  
Masanao Inagaki ◽  
Toshiyuki Kanemasa ◽  
Takaaki Yokota
Keyword(s):  
Adverse Effects ◽  
Adverse Events ◽  
Severe Pain ◽  
Lead Compound ◽  
Inhibitory Effects ◽  
Pharmacokinetic Profiles ◽  
Structure Activity ◽  
The Usa ◽  
Relationship Study ◽  
The Eu

Opioids are widely used for pain management in moderate-to-severe pain. However, opioids are associated with adverse events, such as constipation and emesis/vomiting. To reduce these undesired effects, a structure–activity relationship study of morphinan derivatives was conducted, and a promising lead compound with inhibitory effects on opioid receptors was obtained. Further improvement in the potency and pharmacokinetic profiles of the lead compound led to the discovery of naldemedine, which showed anti-constipation and anti-emetic effects against these adverse events that were induced by morphine without influencing morphine’s analgesic effect. Naldemedine was launched in Japan and the USA in 2017 and in the EU in 2019, for treating opioid-induced constipation.

New Groups of Potential Antituberculotics: Bis(1-aryltetrazol-5-yl) Disulfides. Structure Activity Relationship

1994 ◽  
Vol 59 (1) ◽  
pp. 234-238 ◽  
Author(s):  
Karel Waisser ◽  
Jiří Kuneš ◽  
Alexandr Hrabálek ◽  
Želmíra Odlerová
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Antimycobacterial Activity ◽  
Activity Relationship ◽  
Active Derivative ◽  
Structure Activity ◽  
Medium Activity ◽  
Substituent Constants ◽  
Atypical Strains

Oxidation of 1-aryltetrazole-5-thiols afforded bis(1-aryltetrazol-5-yl) disulfides. The compounds were tested for antimycobacterial activity against Mycobacterium tuberculosis, M. kansasii, M. avium and M. fortuitum. In the case of M. tuberculosis, the logarithm of minimum inhibitory concentration showed a parabolic dependence on hydrophobic substituent constants. Although the compounds exhibited low to medium activity, the most active derivative, bis(4-chlorophenyltetrazol-5-yl) disulfide (III) was more effective against atypical strains than are the commercial tuberculostatics used as standards.

scholarly journals STUDIES OF THE JUGULAR, CAROTID, AND PULMONARY PRESSURES OF ANESTHETIZED DOGS DURING POSITIVE INFLATION OF THE LUNGS

1939 ◽  
Vol 8 (5) ◽  
pp. 553-564 ◽  
Author(s):  
George H. Humphreys ◽  
Richmond L. Moore ◽  
Howard Barkley
Keyword(s):  
Anesthetized Dogs

Effect of two omeprazole doses on gastroesophageal reflux incidence and pH in anesthetized dogs

2019 ◽  
Vol 46 (6) ◽  
pp. 831.e10
Author(s):  
L. Krause ◽  
F. Lotti ◽  
H. Weir ◽  
P. Vogel ◽  
E. Wilcoxen ◽  
...  
Keyword(s):  
Gastroesophageal Reflux ◽  
Anesthetized Dogs

scholarly journals Pharmacodynamic and pharmacokinetic profiles of a neurotensin receptor type 2 (NTS2) analgesic macrocyclic analog

2021 ◽  
Vol 141 ◽  
pp. 111861
Author(s):  
Magali Chartier ◽  
Michael Desgagné ◽  
Marc Sousbie ◽  
Charles Rumsby ◽  
Lucie Chevillard ◽  
...  
Keyword(s):  
Receptor Type ◽  
Neurotensin Receptor ◽  
Pharmacokinetic Profiles
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