Palpitin, an agent of the disopyramide series, was evaluated for its antiarrhythmic potency in the treatment of ventricular and supraventricular arrhythmias and for its effects of ECG and central hemodynamic parameters in 108 patients (91 had coronary heart disease, 8 presented with postmyocardial cardiosclerosis, 5 had hypertensive disease, and 4 suffered from neurocirculatory dystonia). 24-hour ECG monitoring and echocardiography were employed in the study. It was concluded that the drug possessed a high antiarrhythmic potency. No substantial changes were found in the mean values of echocardiographic parameters, as well as of atrioventricular and intraventricular conduction.
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Nat Commun
January 2025
Department of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.
Tetrahydrocannabinol (THC) is the principal psychoactive compound derived from the cannabis plant Cannabis sativa and approved for emetic conditions, appetite stimulation and sleep apnea relief. THC's psychoactive actions are mediated primarily by the cannabinoid receptor CB. Here, we determine the cryo-EM structure of HU210, a THC analog and widely used tool compound, bound to CB and its primary transducer, G.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Biochemistry, National Defense Medical Center, Taipei 114, Taiwan.
Local anesthetics are commonly used in various clinical settings for both prevention and symptom relief. Numerous clinical studies have demonstrated that intra-articular injections of local anesthetics achieve high success rates in orthopedic practices. However, several widely used local anesthetics, including bupivacaine, lidocaine, and ropivacaine, have been shown to exhibit toxicity to chondrocytes, with the underlying mechanisms of chondrotoxicity remaining poorly understood.
View Article and Find Full Text PDFNat Commun
December 2024
Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, China.
By targeting the essential viral RNA-dependent RNA polymerase (RdRP), nucleoside analogs (NAs) have exhibited great potential in antiviral therapy for RNA virus-related diseases. However, most ribose-modified NAs do not present broad-spectrum features, likely due to differences in ribose-RdRP interactions across virus families. Here, we show that HNC-1664, an adenosine analog with modifications both in ribose and base, has broad-spectrum antiviral activity against positive-strand coronaviruses and negative-strand arenaviruses.
View Article and Find Full Text PDFJ Sex Med
January 2025
Andrology and Gender Endocrinology Unit, Department of Experimental Clinical and Biomedical Sciences "Mario Serio", University of Florence, Florence, 50134, Italy.
Background: In males, adenosine (ADO) is known to relax penile smooth muscles, although its role in the vagina is not yet fully elucidated.
Aim: This study investigated the effect of ADO on vagina smooth muscle activity, using a validated female Sprague-Dawley rat model.
Methods: Contractility studies, using noradrenaline-precontracted vaginal strips, tested the effects of ADORA1/3 antagonists and ADORA2A/2B antagonists and agonists.
Cell Mol Life Sci
November 2024
School of Physiology, Pharmacology and Neuroscience, Biomedical Sciences Building, University of Bristol, University Walk, Bristol, BS8 1TD, UK.
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