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The presynaptic component of the serotonergic system is required for clozapine's efficacy.

Clozapine, by virtue of its absence of extrapyramidal side effects and greater efficacy, revolutionized the treatment of schizophrenia, although the mechanisms underlying this exceptional activity remain controversial. Combining an unbiased cheminformatics and physical screening approach, we evaluated clozapine's activity at >2350 distinct molecular targets. Clozapine, and the closely related atypical antipsychotic drug olanzapine, interacted potently with a unique spectrum of molecular targets. This distinct pattern, which was not shared with the typical antipsychotic drug haloperidol, sugges

Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism.

Peripheral cannabinoid receptors exert a powerful inhibitory control over pain initiation, but the endocannabinoid signal that normally engages this intrinsic analgesic mechanism is unknown. To address this question, we developed a peripherally restricted inhibitor (URB937) of fatty acid amide hydrolase (FAAH), the enzyme responsible for the degradation of the endocannabinoid anandamide. URB937 suppressed FAAH activity and increased anandamide levels outside the rodent CNS. Despite its inability to access brain and spinal cord, URB937 attenuated behavioral responses indicative of persistent pa

Schizophrenia-like features in transgenic mice overexpressing human HO-1 in the astrocytic compartment.

Delineation of key molecules that act epigenetically to transduce diverse stressors into established patterns of disease would facilitate the advent of preventive and disease-modifying therapeutics for a host of neurological disorders. Herein, we demonstrate that selective overexpression of the stress protein heme oxygenase-1 (HO-1) in astrocytes of novel GFAP.HMOX1 transgenic mice results in subcortical oxidative stress and mitochondrial damage/autophagy; diminished neuronal reelin content (males); induction of Nurr1 and Pitx3 with attendant suppression of their targeting miRNAs, 145 and 133b

Curcumin Formulations for Better Bioavailability: What We Learned from Clinical Trials Thus Far?

Curcumin has been credited with a wide spectrum of pharmacological properties for the prevention and treatment of several chronic diseases such as arthritis, autoimmune diseases, cancer, cardiovascular diseases, diabetes, hemoglobinopathies, hypertension, infectious diseases, inflammation, metabolic syndrome, neurological diseases, obesity, and skin diseases. However, due to its weak solubility and bioavailability, it has limited potential as an oral medication. Numerous factors including low water solubility, poor intestinal permeability, instability at alkaline pH, and fast metabolism contri

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… that only residues of the unmodified substance were discovered in the liver and kidney. 59 This study also showed that 90% of curcumin was noted in the stomach and small intestine at 30 min while only 1% of curcumin was present after 24 h. 59 Another study revealed that administration of radiolabeled (tritium …

Meeting abstracts from the 21st European Symposium on Radiopharmacy and Radiopharmaceuticals

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… Most potent ligands (Ki < 20 nM) were radiolabeled with tritium using [ 3 H]methyl nosylate. Postmortem human (PD, MSA) brain tissues and α-synuclein fibril-injected mouse brain tissues were used to evaluate specific binding of the radioligands (10nM) by in vitro autoradiography. …

34th Annual Meeting & Pre-Conference Programs of the Society for Immunotherapy of Cancer (SITC 2019): part 2 : National Harbor, MD, USA. 10 November 2019.

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Всемирный конгресс молекулярного воображения 2022.

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… To facilitate quantification, commercial tritium standards were included in all experiments using tritiated ligands, ( [3H]PK11195 and [3H]MK801 for TSPO and NMDA receptors, respectively) while experiments with F18 labeled tracers ([18F]T807 and [18F]Florbetaben for tau and amyloid respectively) were …