ED50
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The significant immune escape of pseudotyped SARS-CoV-2 variant Omicron Open
The emergence of Omicron/BA.1 has brought new challenges to fight against SARS-CoV-2. A large number of mutations in the Spike protein suggest that its susceptibility to immune protection elicited by the existing COVID-19 infection and vac…
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Insecticidal Activity and Insect Repellency of Four Species of Sea Lily (Comatulida: Comatulidae) From Taiwan Open
The methanol and ethyl acetate (EA) extracts of four species of sea lily (Himerometra magnipinna, Comaster multifidus, Comanthina sp., and Comatella maculata) were evaluated for their insecticidal activity against Yellow-fever mosquito lar…
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Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and<i>in vivo</i>studies Open
Twelve new derivatives of benzothiazole bearing benzenesulphonamide and carboxamide were synthesised and investigated for their in vivo anti-inflammatory, analgesic and ulcerogenic activities. Molecular docking showed an excellent binding …
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Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives as Potential Anticonvulsant Agents Open
New benztriazoles with a mercapto-triazole and other heterocycle substituents were synthesized and evaluated for their anticonvulsant activity and neurotoxicity by using the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPT…
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Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1-phenylpyrazolo[3,4-<i>d</i>]pyrimidine derivatives Open
A new group of 1-phenylpyrazolo[3,4-d]pyrimidine derivatives 14a-d-21 were synthesized from 2-(6-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)acetohydrazide (12). All the synthesized compounds were evaluated for their cyclooxygenase…
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BN‐9, a chimeric peptide with mixed opioid and neuropeptide FF receptor agonistic properties, produces nontolerance‐forming antinociception in mice Open
Background and Purpose Neuropeptide FF (NPFF) behaves as an endogenous opioid‐modulating peptide. In the present study, the opioid and NPFF pharmacophore‐containing chimeric peptide BN‐9 was synthesized and pharmacologically characterized.…
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When less is more – efficacy with less toxicity at the ED50 Open
The individualization of drug dosage to maximize benefit and minimize risk is always a challenge since desired benefit is often associated with many dose-related adverse effects. Most disease is subacute and mild to moderate in severity. D…
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Multifunctional Hybrid Compounds Derived from 2-(2,5-Dioxopyrrolidin-1-yl)-3-methoxypropanamides with Anticonvulsant and Antinociceptive Properties Open
The focused set of new pyrrolidine-2,5-diones as potential broad-spectrum hybrid anticonvulsants was described. These derivatives integrate on the common structural scaffold the chemical fragments of well-known antiepileptic drugs such as …
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Synthesis and anticonvulsant activities of novel 2-(cyclopentylmethylene)hydrazinyl-1,3-thiazoles in mouse models of seizures Open
Synthesis, characterization and investigation of in vivo anticonvulsant activities of 13 novel cyclopentanecarbaldehyde-based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using (1)H and (13)C NMR, FAB(+)-…
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Green Synthesis of Zinc Oxide Nanoparticles via Algal Route and its Action on Cancerous Cells and Pathogenic Microbes Open
Application of metal oxide nanoparticles for treatment of melanoma cells and microbes is being investigated. Zinc oxide nanoparticles (ZnO NPs) deserve special mention where particles cause destruction of melanoma cells with minimal damage…
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Ascorbic acid therapy: A potential strategy against comorbid depression-like behavior in streptozotocin-nicotinamide-induced diabetic rats Open
This study examined the potency and efficacy of ascorbic acid (AA) in the management of depression-like behavior in diabetic rats. Diabetes mellitus was induced by single intraperitoneal injections of nicotinamide (120 mg/kg) and streptozo…
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ED50 of propofol in combination with low‐dose sufentanil for intravenous anaesthesia in hysteroscopy Open
Objectives Sufentanil has favourable pharmacodynamic and pharmacokinetic properties as an opioid, and it is usually co‐administered with propofol as intravenous anaesthesia for hysteroscopic examination or therapeutic surgery. However, the…
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An evaluation of the anti-inflammatory, antipyretic and analgesic effects of hydroethanol leaf extract of<i>Albizia zygia</i>in animal models Open
The results suggest that AZE possesses anti-inflammatory, antipyretic and analgesic properties, which justifies its traditional use. Also, the results show the involvement of the opioidergic, adenosinergic and the muscarinic cholinergic pa…
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Synthesis, Anticonvulsant and Antinociceptive Activity of New Hybrid Compounds: Derivatives of 3-(3-Methylthiophen-2-yl)-pyrrolidine-2,5-dione Open
The present study aimed to design and synthesize a new series of hybrid compounds with pyrrolidine-2,5-dione and thiophene rings in the structure as potential anticonvulsant and antinociceptive agents. For this purpose, we obtained a serie…
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Acute and chronic effects of cannabidiol on Δ⁹-tetrahydrocannabinol (Δ⁹-THC)-induced disruption in stop signal task performance. Open
Recent clinical and preclinical research has suggested that cannabidiol (CBD) and Δ9-tetrahydrocannabinol (Δ9-THC) have interactive effects on measures of cognition; however, the nature of these interactions is not yet fully characterized.…
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Antinociceptive Effects of Prim-O-Glucosylcimifugin in Inflammatory Nociception via Reducing Spinal COX-2 Open
We measured anti-nociceptive activity of prim-o-glucosylcimifugin (POG), a molecule from Saposhnikovia divaricate (Turcz) Schischk. Anti-nociceptive or anti-inflammatory effects of POG on a formalin-induced tonic nociceptive response and a…
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Anticonvulsant Effect of the Aqueous Extract and Essential Oil of Carum Carvi L. Seeds in a Pentylenetetrazol Model of Seizure in Mice. Open
This study showed that the aqueous extract and essential oil of caraway had anticonvulsant properties. However, the essential oil was more potent and effective than was the aqueous extract as an anticonvulsant. Additionally, the anticonvul…
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Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure–Activity Relationship of Triazine–4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice Open
Here, we report analgesic and anti-inflammatory activity of a series of compounds obtained by appending 4-aminophenylmorpholin-3-one and acyclic, cyclic, or heterocyclic moieties on 1,3,5-triazine. The structures of compounds 4b and 6b are…
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Antiseizure drug efficacy and tolerability in established and novel drug discovery seizure models in outbred vs inbred mice Open
Objective Initial identification of new investigational drugs for the treatment of epilepsy is commonly conducted in well‐established mouse acute and chronic seizure models: for example, maximal electroshock (MES), 6 Hz, and corneal kindli…
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The new algorithm for calculation of median lethal dose (LD<sub>50</sub>) and effective dose fifty (ED<sub>50</sub>) of Micrarus fulvius venom and anti-venom in mice Open
One million people throughout the world are bitten yearly by poisonous snakes. Of this, one-tenth died and three-tenth suffer some forms of disabilities. In view of this, anti-snake venoms are currently being developed against viper and co…
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N-Benzyl-(2,5-dioxopyrrolidin-1-yl)propanamide (AS-1) with Hybrid Structure as a Candidate for a Broad-Spectrum Antiepileptic Drug Open
In our recent studies, we identified compound N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide (AS-1) as a broad-spectrum hybrid anticonvulsant which showed potent protection across the most important animal acute seizure models such as th…
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Pharmacological Properties of Riparin IV in Models of Pain and Inflammation Open
Riparins, natural alkaloids of the alkamide group, can be synthesized by simple methods, enhancing their potential application in pharmaceutical development. Here, the pharmacological properties of riparins were investigated in in vitro an…
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Efficacy of mGlu<sub>2</sub>‐positive allosteric modulators alone and in combination with levetiracetam in the mouse 6 Hz model of psychomotor seizures Open
Summary Objective The metabotropic glutamate receptor subtype 2 ( mG lu 2 ) possesses both orthosteric and allosteric modulatory sites, are expressed in the frontal cortex and limbic structures, and can affect excitatory synaptic transmiss…
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Behavioral and Biochemical Evidences for Antidepressant-Like Activity of Celastrus Paniculatus Seed Oil in Mice. Open
Celastrus paniculatus seed oil produced significant antidepressant-like effect in mice possibly through interaction with dopamine D2, serotonergic, and GABAB receptors; as well as inhibition of MAO-A activity and decrease in plasma cortico…
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Comparative Pharmacological Effects of Lisuride and Lysergic Acid Diethylamide Revisited Open
Lisuride is a non-psychedelic serotonin (5-HT) 2A receptor (5-HT2A) agonist and analogue of the psychedelic lysergic acid diethylamide (LSD). Lisuride also acts as an agonist at the serotonin 1A receptor (5-HT1A), a property known to count…
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Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists Open
In previous work, we discovered a lead compound and conducted initial SAR studies on a novel series of dioxotriazines to identify the compound as one of the P2X3 receptor antagonists. This compound showed high P2X3 receptor selectivity and…
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Eutylone and Its Structural Isomers Interact with Monoamine Transporters and Induce Locomotor Stimulation Open
Synthetic cathinones are a class of new psychoactive substances that induce psychostimulant effects and pose risk for hospitalizations, overdose, and death. At the present time, derivatives of the synthetic cathinone, methylone, are being …
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Lung protective effects of dietary malate esters derivatives from Bletilla striata against SiO2 nanoparticles through activation of Nrf2 pathway Open
The dietary malate esters derivatives of B. striata could significantly increase the viability of nm SiO2-induced A549 cells and decrease the finer particles-induced cell damages. Militarine is especially promising compound for chemopreven…
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Synthesis, cyclooxygenase inhibition and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1<i>H</i>-pyrazole derivatives possessing methanesulphonyl pharmacophore Open
A new series of 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives 13a-p were synthesized via aldol condensation of 3/4-nitroacetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-metha…
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Co-administration of Pregabalin and Curcumin Synergistically Decreases Pain-Like Behaviors in Acute Nociceptive Pain Murine Models Open
Analgesic drugs in a combination-form can achieve greater efficacy with lesser side effects compared to either drug alone. The combination of drugs acting at different targets or mechanisms of action has been recognized as an alternative a…