Piperazine derivatives were screened using the ChEMBL database, paving the way for the design, synthesis, and evaluation of a novel series of dual COX-2/5-LOX inhibitors and identifying their role in mitigating cancer cell proliferation. Compound 9d with 4-Cl substitution at the terminal phenyl ring showed promising inhibition of COX-2 (IC50 = 0.25 ± 0.03 μM)… Continue reading Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity
Tag: Neuropharmacology and Drugs
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity
Piperazine derivatives were screened using the ChEMBL database, paving the way for the design, synthesis, and evaluation of a novel series of dual COX-2/5-LOX inhibitors and identifying their role in mitigating cancer cell proliferation. Compound 9d with 4-Cl substitution at the terminal phenyl ring showed promising inhibition of COX-2 (IC50 = 0.25 ± 0.03 μM)… Continue reading Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity
Central control of opioid-induced mechanical hypersensitivity and tolerance in mice
Yin et al. found that intra-PBN injection of morphine or DAMGO paradoxically induces bilateral morphine-resistant mechanical pain hypersensitivity instead of relieving mechanical pain. Further, they identified a brain-to-spinal opioid pathway that controls morphine-induced mechanical OIH and analgesic tolerance. Targeting this opioid pathway rescued repetitive systemic morphine-induced mechanical OIH/tolerance in mice.
A perspective on Alzheimer’s disease: exploring the potential of terminal/paradoxical lucidity and psychedelics
The way sensory prediction changes under anesthesia tells us how conscious cognition works
Our brains constantly work to make predictions about what’s going on around us to ensure that we can attend to and consider the unexpected, for instance. A new study examines how this works during consciousness and also breaks down under general anesthesia. The results add evidence to the idea that conscious thought requires synchronized communication… Continue reading The way sensory prediction changes under anesthesia tells us how conscious cognition works
[ASAP] Discovery of Orally Active Phenylquinoline-Based Soluble Epoxide Hydrolase Inhibitors with Anti-Inflammatory and Analgesic Activity
[ASAP] Molecular Mechanisms of Methamphetamine-Induced Addiction via TAAR1 Activation
[ASAP] The Interplay between MiR-134/BDNF and LKB1/AMPK/SIRT1 Accentuates the Antidepressant Efficacy of Empagliflozin in Ovariectomized Rats
Antidepressants Linked to Improved Verbal Memory
Two antidepressants appeared to improve verbal memory in moderate to severe depression, an effect linked to changes in serotonin 5-HT4 receptor levels as shown on PET. Medscape Medical News
Startup helps people fall asleep by aligning audio signals with brainwaves
AI SummaryElemind, a startup founded by a team including an MIT professor, is using an EEG headband to emit acoustic stimulation aligned with brainwaves to help people fall asleep more quickly. In a study, 30 minutes of stimulation decreased sleep onset by 10 to 15 minutes. The device may offer benefits over sleeping pills in… Continue reading Startup helps people fall asleep by aligning audio signals with brainwaves