The effect of cannabinoids on motion-induced emesis is unknown. The present study investigated the action of phytocannabinoids against motion-induced emesis in Suncus murinus. Suncus murinus were injected intraperitoneally with either cannabidiol (CBD) (0.5, 1, 2, 5, 10, 20 and 40 mg/kg), Delta(9)-tetrahydrocannabinol (Delta(9)-THC; 0.5, 3, 5 and 10 mg/kg) or vehicle 45 min. before exposure to ...

Retrograde synaptic signaling by endogenous cannabinoids (endocannabinoids) is a recently discovered form of neuromodulation in the brain. In the basolateral amygdala (BLA), endocannabinoid signaling has been implicated in learning and memory, specifically in extinction of aversive memories. To examine retrograde endocannabinoid signaling in this brain region, BLA neurons were freshly isolated ...

A facile and convenient synthesis of new heterocyclic compounds containing a sulfamoyl moiety suitable for use as antimicrobial agents was reported. The precursor 3-oxo-3-phenyl-N-(4-sulfamoylphenyl)propionamide was coupled smoothly with arenediazonium salt producing hydrazones which reacted with malononitrile or triethylorthoformate affording pyridazine and triazine derivatives, respectively. ...

Inhibition of cannabinoid receptor 1 (CB1) has shown efficacy in reducing body weight and improving metabolic parameters, with the effects correlating with target engagement in the brain. The peripheral effects of inhibiting the CB1 receptor has been appreciated through studies in diet-induced obese and liver-specific CB1 knockout mice. In this article, we systematically investigated gene expre...

In the title dinuclear compound, [Zn(2)(C(6)H(6)N(3)O)(2)(C(6)H(7)N(3)O)(2)](NO(3))(2), the Zn(II) cation is N,N'-chelated by one pyridine-2-carboxamide oximate anion and one pyridine-2-carboxamide oxime mol-ecule, and is further bridged by an oxime O atom from the adjacent pyridine-2-carboxamide oximate anion, forming a distorted trigonal bipyramidal coordination. Two pyridine-2-carboxamide ox...

4-Amino-5-imidazolecarboxamide (l), an amine found to accumulate in bacterial systems poisoned either by sulfonamides (2, 3) or aminopterin (4), has been suggested as an intermediate of purine synthetic reactions (5, 6). Although the metabolic inertness of the carboxamide’ in certain bacterial systems (7, 8) led to the belief by some (8) that this compound was an aberrant product of metabolism ...

ABSTRACT. The inhibition of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro) and papain-like (PLpro) prevents viral multiplications. Molecular docking, absorption, distribution, metabolism, excretion, toxicity (ADMET) studies pyrazole-indole molecules 6a, b, Schiff bases 8a, pyrazolo[1,5-a]pyrimidines 10a, b were performed done. Based on the molecular docking st...

The in vitro effects of arachidonyl-2-chloroethylamide (ACEA; a selective CB(1)-receptor agonist) and N-piperidin-l-yl)-5-(4-chlorophenyl)-1-(2,4-cochlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A; a selective CB(1)-receptor antagonist) on lipid peroxidation (spontaneous and Fe (2+)-induced), total glutathione (GSH)-level and activity of antioxidant enzymes (superoxide dismutase, glu...

The measles virus (MeV), a member of the paramyxovirus family, is an important cause of pediatric morbidity and mortality worldwide. In an effort to provide therapeutic treatments for improved measles management, we previously identified a small, non-nucleoside organic inhibitor of the viral RNA-dependent RNA polymerase by means of high-throughput screening. Subsequent structure-activity relati...

Endocannabinoid release from a single neuron has been shown to cause presynaptic inhibition of transmitter release at many different sites. Here, we demonstrate that hypothalamic proopiomelanocortin (POMC) neurons release endocannabinoids continuously under basal conditions, unlike other release sites at which endocannabinoid production must be stimulated. The basal endocannabinoid release sele...