No catalyst required! A highly efficient, catalyst‐free process to generate diimide in situ from hydrazine monohydrate and molecular oxygen for the selective reduction of alkenes has been developed. The use of a gas–liquid segmented flow system allowed safe operating conditions and dramatically enhanced this atom‐economical reaction, resulting in short processing times.
Rationale
Pulmonary hypertension (PH) is characterized by pulmonary vascular remodeling that leads to pulmonary congestion, uncompensated right-ventricle (RV) failure, and premature death. Preclinical studies have demonstrated that the G protein-coupled estrogen receptor (GPER) is cardioprotective in male rats and that its activation elicits vascular relaxation in rats of either sex.
Objectives
To study the effects of GPER on the cardiopulmonary system by the administration of its selective agonist G1 in male rats with monocrotaline (MCT)-induced PH.
Methods
Rats received a single intraperitoneal injection of MCT (60 mg/kg) for PH induction. Experimental groups were as follows: control, MCT + vehicle, and MCT + G1 (400 μg/kg/day subcutaneous). Animals (n = 5 per group) were treated with vehicle or G1 for 14 days after disease onset.
Measurements and main results
Activation of GPER attenuated exercise intolerance and reduced RV overload in PH rats. Rats with PH exhibited echocardiographic alterations, such as reduced pulmonary flow, RV hypertrophy, and left-ventricle dysfunction, by the end of protocol. G1 treatment reversed these PH-related abnormalities of cardiopulmonary function and structure, in part by promoting pulmonary endothelial nitric oxide synthesis, Ca2+ handling regulation and reduction of inflammation in cardiomyocytes, and a decrease of collagen deposition by acting in pulmonary and cardiac fibroblasts.
Conclusions
G1 was effective to reverse PH-induced RV dysfunction and exercise intolerance in male rats, a finding that have important implications for ongoing clinical evaluation of new cardioprotective and vasodilator drugs for the treatment of the disease.
The forced degradation of 11 ibuprofen tablet brands was carried out according to current industry best practices. The results indicated an incompatibility between ibuprofen and two common tablet excipients (polyethylene glycol and polysorbate 80) that were observed to accelerate the degradation of ibuprofen in tablets stored for three weeks at 70°C/75% RH. Studies of binary drug/excipient samples supported the conclusion. One degradant that was observed at increased levels was 4-isobutylacetophenone (4-IBAP), which is a known toxin.
Katalysator? Wozu! Ein hoch effizienter katalysatorfreier Prozess zur In‐situ‐Erzeugung von Diimid aus Hydrazin‐Monohydrat und molekularem Sauerstoff für die selektive Reduktion von Alkenen wurde entwickelt. Ein System mit segmentiertem Gas‐Flüssigkeits‐Strom garantiert sichere Arbeitsbedingungen und beschleunigt die atomökonomische Reaktion so stark, dass eine kurze Prozessdauer ausreicht.
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