The new sigma ligand cis-(±)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl) methyl]-1-(4-methylphenyl) cyclopropanecarboxylate [(±)-PPCC] is a promising tool for the treatment of various diseases. With the aim to investigate the absorption of (±)-PPCC by the cell membranes, in this study we evaluated the influence on thermotropic behavior of membrane model exerted by PPCC both as free base or as oxalic salt. To fulfill this purpose differential scanning calorimetry was used. The findings highlight that PPCC affects the thermodynamic parameters of phospholipids in different manner depending on whether it is in the salt or base form as well as function of the amount of drugs dispersed in the lipid matrix. The salt form of PPCC was uptaken by the membrane model faster than the free base. In addition, preliminary information on the use of a lipophilic carrier for PPCC was obtained.
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http://dx.doi.org/10.1016/j.ijpharm.2014.04.052 | DOI Listing |
Acc Chem Res
January 2025
Department of Chemistry, University at Buffalo, State University of New York, Buffalo, New York 14260, United States.
ConspectusUnderstanding f element-ligand covalency is at the center of efforts to design new separations schemes for spent nuclear fuel, and is therefore of signficant fundamental and practical importance. Considerable effort has been invested into quantifying covalency in f element-ligand bonding. Over the past decade, numerous studies have employed a variety of techniques to study covalency, including XANES, EPR, and optical spectroscopies, as well as X-ray crystallography.
View Article and Find Full Text PDFProg Neuropsychopharmacol Biol Psychiatry
January 2025
Louisiana State University, Department of Comparative Biomedical Sciences, Baton Rouge, LA 70803, United States of America. Electronic address:
Renewed interest in the clinical use of psychedelic drugs acknowledges their therapeutic effectiveness. It has also provided a changing frame of reference for older psychedelic drug study data, especially regarding concentrations of N, N-dimethyltryptamine (DMT) reported in rodent brains and recent discoveries in DMT receptor interactions in rat brain neurons and select brain areas. The mode of action of DMT in its newly defined role as a neuroplastogen, its effectiveness in treating neuropsychiatric disorders, and its binding to intracellular sigma-1 and 5HT2a receptors may define these possible roles.
View Article and Find Full Text PDFJ Am Chem Soc
January 2025
School of Chemistry, Dalian University of Technology, No. 2 Linggong Rd., 116024 Dalian, Liaoning, China.
Activation of N through transition-metal complexes has emerged as a powerful strategy for N fixation under mild conditions. Dissociative route and associative route are considered as two major routes for N transformation on transition-metal complexes. Homolysis of N between two metal fragments is the crucial step of the dissociative route and has been proven to be an efficient approach to the terminal metal nitride, which is the key intermediate for both routes.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
Freie Universitat Berlin, Chemistry and Biochemistry, Fabeckstraße 34-36, 14195, Berlin, GERMANY.
Neutral mesoionic carbenes (MICs) based on a 1,2,3-triazole core have had a strong impact on various branches of chemistry such as homogeneous catalysis, electrocatalysis, and photochemistry/photophysics. We present here the first general synthesis of anionic mesoionic carbenes (anMICs) based on a 1,2,3-triazole core and a borate backbone. The free anMIC is stable in solution under an inert atmosphere at low temperatures, and can be stored for several weeks.
View Article and Find Full Text PDFACS Pharmacol Transl Sci
January 2025
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Sigma 1 receptor (S1R) is a multifunctional, ligand-activated protein located in the membranes of the endoplasmic reticulum (ER). It mediates a variety of neurological disorders, including epilepsy, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease. The wide neuroprotective effects of S1R agonists are achieved by a variety of pro-survival and antiapoptotic S1R-mediated signaling functions.
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