Pharmacokinetics of a novel nootropic agent, alaptide, have been examined in plasma and brain of mice, rats and rabbits following an intravenous dose (1 mg kg-1). First-order equilibration rate constants between plasma and brain (kBO) were calculated by a two-compartment model with a linked compartment (brain). Brain alaptide equilibrates rapidly with the central compartment in mice and rats due to the high kBO/beta ratio. In rabbits the equilibration is much slower (kBO/beta approximately 1). Partition coefficients between brain and plasma calculated from areas under the brain and plasma concentration-time curves, are 0.479, 0.549 and 0.864, in mice, rats and rabbits, respectively.
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http://dx.doi.org/10.1111/j.2042-7158.1991.tb03200.x | DOI Listing |
Acta Med Philipp
December 2024
PT Prodia StemCell Indonesia (ProSTEM), Jakarta, Indonesia.
Background And Objectives: Intraperitoneal injection (i.p.) of D-galactose (D-gal) accelerates aging and develops aging models.
View Article and Find Full Text PDFWe recently reported that a chimeric peptide (GEP44) targeting the glucagon-like peptide-1 receptor (GLP-1R) and neuropeptide Y1- and Y2-receptors decreased body weight (BW), energy intake and core temperature in diet-induced obese (DIO) male and female mice. Given that GEP44 was found to reduce core temperature (surrogate measure of energy expenditure (EE)) in DIO mice, we hypothesized that GEP44 would reduce EE in male and female high fat diet (HFD)-fed rats. To test this, rats were maintained on a HFD for at least 4 months to elicit DIO prior to undergoing a sequential 2-day vehicle period, 2-day GEP44 (50 nmol/kg) period and a minimum 2-day washout period and detailed measures of energy homeostasis.
View Article and Find Full Text PDFJ Pharmacol Sci
February 2025
Department of Physical Chemistry for Bioactive Molecules, Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, 985-1 Sanzo, Higashimura-cho, Fukuyama, Hiroshima, 729-0292, Japan.
The purpose of the present study is to investigate changes in the kynurenine pathway after intracerebral hemorrhage (ICH) and its effects on ICH-induced injury. The exposure of a primary rat microglial culture to thrombin increased the mRNA level of kynurenine 3-monooxygenase (KMO), and this increase was attenuated by a p38 MAPK inhibitor. Thrombin also increased the protein level of KMO.
View Article and Find Full Text PDFJ Ethnopharmacol
January 2025
College of Pharmacy, Shenzhen Technology University, Shenzhen 518118, Guangdong, China; Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai 90112, Songkhla, Thailand; Drug Delivery System Excellence Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai 90112, Songkhla, Thailand. Electronic address:
Ethnopharmacological Relevance: Fagonia bruguieri var. laxa Boiss., also known as Dhamansa or Dhamaran, is a well-known xerophyte traditionally used for managing pain, inflammation, fever, and related disease conditions.
View Article and Find Full Text PDFJ Sport Health Sci
January 2025
Institute of Cardiovascular Sciences, Shanghai Engineering Research Center of Organ Repair, Joint International Research Laboratory of Biomaterials and Biotechnology in Organ Repair (Ministry of Education), School of Life Science, Shanghai University, Shanghai 200444, China; Cardiac Regeneration and Ageing Lab, Institute of Geriatrics (Shanghai University), Affiliated Nantong Hospital of Shanghai University (The Sixth People's Hospital of Nantong), School of Medicine, Shanghai University, Nantong 226011, China. Electronic address:
Background: Exercise induces molecular changes that involve multiple organs and tissues. Moreover, these changes are modulated by various exercise parameters-such as intensity, frequency, mode, and duration-as well as by clinical features like gender, age, and body mass index (BMI), each eliciting distinct biological effects. To assist exercise researchers in understanding these changes from a comprehensive perspective that includes multiple organs, diverse exercise regimens, and a range of clinical features, we developed Exercise Regulated Genes Database (ExerGeneDB), a database of exercise-regulated differential genes.
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