New deaza derivatives of anpirtoline have been synthesized by three different methods. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied.
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http://dx.doi.org/10.1002/(sici)1521-4184(19991)332:1<13::aid-ardp13>3.0.co;2-l | DOI Listing |
Trials
January 2025
Department of Anesthesiology, West China Hospital, Sichuan University, Chengdu, China.
Background: Surgical intervention is critical in the treatment of hip developmental dysplasia in children. Perioperative analgesia, usually based on high opioid dosages, is frequently used in these patients. In some circumstances, regional anesthetic procedures such as caudal block and lumbar plexus block have also been used.
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January 2025
Institute of Drug Metabolism and Pharmaceutical Analysis, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.
Freeze drying is one of the common methods to extend the long-term stability of biologicals. Biological products in solid form have the advantages of convenient transportation and stable long-term storage. However, long reconstitution time and extensive visible bubbles are frequently generated during the reconstitution process for many freeze-dried protein formulations, which can potentially affect the management efficiency of staff, patient compliance, and product quality.
View Article and Find Full Text PDFAAPS PharmSciTech
January 2025
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576104, India.
The transdermal route is one of the effective routes for delivering drugs. It also overcomes many limitations associated with oral delivery. One of the limitations of this route is the drug's poor skin permeability-stratum corneum, the skin's outermost layer that also acts as a barrier for the drug to penetrate.
View Article and Find Full Text PDFSci Rep
January 2025
Department of Pesticide Chemistry, National Research Centre, Dokki, 12622, Giza, Egypt.
Chemoprevention is one of the accessible strategies for preventing, delaying or reversing cancer processing utilizing chemical intervention of carcinogenesis. NAD(P)H quinone oxidoreductase 1 (NQO1) is a xenobiotic metabolizing cytosolic enzyme/protein with important functional properties towards oxidation stress, supporting its ability in detoxification/chemoprotective role. A set of 3,5-diylidene-4-piperidones (as curcumin mimics) bearing alkyl sulfonyl group were synthesized with potential NQO1 induction properties.
View Article and Find Full Text PDFPLoS One
January 2025
Dept. of Psychiatry, Harvard Medical School, McLean Hospital, Belmont, Massachusetts, United States of America.
Opioid dependence is defined by an aversive withdrawal syndrome upon drug cessation that can motivate continued drug-taking, development of opioid use disorder, and precipitate relapse. An understudied but common opioid withdrawal symptom is disrupted sleep, reported as both insomnia and daytime sleepiness. Despite the prevalence and severity of sleep disturbances during opioid withdrawal, there is a gap in our understanding of their interactions.
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