In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinities aimed at producing compounds with good pharmacokinetics properties and in vivo efficacy in rat models of gastric acid and pancreatic amylase secretion.
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http://dx.doi.org/10.1016/j.bmcl.2009.09.065 | DOI Listing |
Prog Neuropsychopharmacol Biol Psychiatry
December 2024
Laboratório de Avaliações Farmacológicas e Toxicológicas Aplicadas às Moléculas Bioativas (LaftamBio Pampa), Universidade Federal do Pampa, Itaqui, RS, Brazil. Electronic address:
Amphetamine (AMPH) abuse represents a major global public health issue, highlighting the urgent need for effective therapeutic interventions to manage addiction caused by this psychostimulant. This study aimed to assess the potential of m-trifluoromethyl-diphenyldiselenide [(m-CF-PhSe)] in preventing the addictive effects induced by AMPH through targeting dopamine metabolism proteins. (m-CF-PhSe) is of interest due to its demonstrated efficacy in mitigating opioid abuse, establishing it as a promising candidate for addiction treatment research.
View Article and Find Full Text PDFJ Ethnopharmacol
December 2024
Key Laboratory of Xin'an Medicine, Ministry of Education, Anhui University of Chinese Medicine, Hefei, Anhui, PR China, 230038; Institute of Surgery, Anhui Academy of Chinese Medicine, Anhui University of Chinese Medicine, Hefei, Anhui, PR China, 230038. Electronic address:
Ethnopharmacological Relevance: Type 2 diabetes mellitus (T2DM) is a metabolic disease that can lead to complications affecting multiple organs, including the liver. Gegen Qinlian Decoction (GQD) has demonstrated considerable efficacy in the management of T2DM and its complications in accordance with the tenets of modern Chinese medicine. However, the molecular mechanism by which GQD alleviates diabetic liver injury is unclear.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Radiation Biology Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA), Cairo, Egypt.
Globally, traumatic injuries and severe hemorrhagic wounds resulting from natural disasters, wars, traffic accidents, and operation rooms, especially during birth, are among the most difficult humanitarian and economic problems. Thus, the priority in emergency medical treatment is reducing unexpected blood loss, which can significantly influence a patient's rescue and recovery speed. For the immediate cessation of bleeding in severe hemorrhagic wounds and to speed up their healing, environmentally friendly γ-ionizing irradiation technology was used to develop innovative natural-based hydrogels impregnated with traditional medicinal plant extracts (MPE) with proven hemostatic and bactericidal potential as potential dressings for hemostasis, infection control, and wound healing.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Swiss Tropical and Public Health Institute, Kreuzstrasse 2, 4123, Allschwil, Switzerland; University of Basel, P.O. Box CH-4003, Basel, Switzerland. Electronic address:
For over three decades, praziquantel (PZQ) has been the mainstay chemotherapy for prevention and treatment of schistosomiasis. The excessive use of PZQ, coupled with the lack of advanced drug candidates in the current anti-schistosomiasis drug development pipeline, emphasizes the genuine need for new drugs. In the current work, we investigated the antischistosomal potential of a new series of compounds derived from the privileged benzimidazole scaffold, which exhibited low micromolar IC potency in the range of 1.
View Article and Find Full Text PDFAppl Biochem Biotechnol
December 2024
Department of Biotechnology, Science Campus, Alagappa University, Karaikudi, India.
Early childhood caries (ECC), a severe form of dental caries, is exacerbated by the synergistic interaction between Streptococcus mutans and Candida albicans, leading to greater disease severity than their individual effects. This underscores the need for more targeted and potent therapeutic alternatives. Given the promising anti-infective properties of quaternary ammonium surfactants (QAS), this study explores the microbicidal properties of one such QAS, cetyltrimethylammonium chloride (CTAC), against both individual- and dual-species cultures of S.
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