1-[1-(2-Benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (BTCP) and cocaine bind to the neuronal dopamine transporter (DAT) to strongly inhibit dopamine (DA) reuptake. Although similar to acute administration, cocaine and BTCP produce sensitization and tolerance, respectively, on chronic administration. We previously found that liver microsomes produced two primary metabolites from BTCP with a high affinity for DAT. Because such metabolites, if produced in vivo, could account for the pharmacological difference with cocaine, it was important to compare BTCP biotransformations in vitro and in vivo. Therefore, we identified and quantified BTCP and primary metabolites in mice urine, plasma, and brain after acute i.p. administration. The low recovery yield suggest that BTCP might behave like its close analogue, phencyclidine, with long-term storage of metabolites. Two active metabolites found in vitro were found in mice brain with estimated half-life values similar to that of BTCP ( approximately 0.3 h). Although respective brain concentrations were 20 and 40 times lower than that of BTCP, their potency to displace in vivo [3H]BTCP bound to the DAT was 50 and 10 times higher, respectively, than that of BTCP. They could, therefore, contribute to the inhibition of DA transport and play an important role in BTCP pharmacology. They could also explain the differences between BTCP and cocaine on repeated administration.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/s0928-0987(99)00077-9 | DOI Listing |
Adv Biotechnol (Singap)
February 2024
State Key Laboratory of Traditional Chinese Medicine/School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, 510006, China.
Mass spectrometry imaging (MSI) serves as a valuable tool enabling researchers to scrutinize various compounds, peptides, and proteins within a sample, providing detailed insights at both elemental and molecular levels. This innovative technology transforms information obtained from a mass spectrometer- encompassing ionic strength, mass-to-charge ratio, and ionized molecule coordinates-within a defined region into a pixel-based model. Consequently, it reconstructs the spatial distribution of ions, allowing for a comprehensive understanding of molecular landscapes.
View Article and Find Full Text PDFTree Physiol
January 2025
Centre for Environmental and Marine Studies (CESAM), Department of Biology, University of Aveiro, Campus Universitário de Santiago, Aveiro 3810-193, Portugal.
Ink disease caused by the hemibiotrophic root pathogen Phytophthora cinnamomi (Pc) is devastating for the European chestnut (Castanea sativa), unlike Asian chestnuts and interspecific hybrids which are resistant to Pc. The role that hormone responses play for Pc resistance remains little understood, especially regarding the temporal regulation of hormone responses. We explored the relationship between changes in tree health and physiology and alterations in leaf and root phytohormones and primary and secondary metabolites during compatible and incompatible Castanea spp.
View Article and Find Full Text PDFFront Med (Lausanne)
January 2025
Department of Integrated Traditional Chinese Medicine (TCM) and Western Medicine, Shanghai First Maternity and Infant Hospital, School of Medicine, Tongji University, Shanghai, China.
Introduction: Recurrent spontaneous abortion (RSA) represents a significant clinical challenge, with its underlying mechanisms yet to be fully elucidated. Despite advances in understanding, the precise pathophysiology driving RSA remains unclear. Angelica sinensis, a traditional herbal remedy, is frequently used as an adjunctive treatment for miscarriage.
View Article and Find Full Text PDFScand J Clin Lab Invest
January 2025
Section of Clinical Biochemistry, University of Verona, Verona, Italy.
Crystals in urinary sediment are commonly recognized structures, typically identified by a combination of crystal morphology and urine pH. In this paper, we present the first reported case of EDDP (2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidene) crystals, the primary metabolite of methadone, in a 67-year-old male with hepatorenal syndrome. Routine urinalysis revealed numerous needle-shaped crystals, which prompted further investigation.
View Article and Find Full Text PDFSci Rep
January 2025
Division of Human Nutrition and Health, Wageningen University, Stippeneng 4, 6708 WE, Wageningen, The Netherlands.
Cannabidiol (CBD), a specialized metabolite (phytocannabinoid) abundant in Cannabis sativa, is attracting increasing attention for its alleged health-promoting properties. The present study aimed to investigate the pharmacokinetics of CBD and its primary metabolite, 7-hydroxy-cannabidiol (7-OH-CBD), following a single oral dose of a CBD-rich Cannabis sativa extract, equivalent to 70 mg CBD, in healthy male (n=5) and female (n=6) participants. Using a randomized crossover design, the study evaluated the impact of a standardized high-fat meal compared to fasting on the oral bioavailability of CBD.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!