The distribution of muscarinic ACh receptors was studied autoradiographically in cryostat sections of the pigeon telencephalon using 3H-Quinuclidinylbenzylate (QNB) as a ligand. Highest receptor density was observed in the hyperstriatum ventrale, palaeostriatum augmentatum, septum, and parts of the archistriatum In sites of known sensory input of neostriatum (field L) and ectostriatum low receptor binding was observed. Acetylcholinesterase distribution is in good agreement with the receptor picture only in the basal telencephalon. In the pallium differences in the pattern of these two components can be seen.
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Arch Insect Biochem Physiol
January 2025
Department of Entomology, College of Plant Protection, China Agricultural University, Beijing, China.
Cyclaniliprole, a type of the third-generation anthranilic diamide insecticide, was mainly used for management of various pests. Myzus persicae (Hemiptera: Aphididae), known as the peach-potato aphid, is an economically essential pest with worldwide distribution. However, the risk assessment of cyclaniliprole in M.
View Article and Find Full Text PDFMolecules
January 2025
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Trg Marka Marulića 19, HR-10 000 Zagreb, Croatia.
Considering our previous experience in the design of new cholinesterase inhibitors, especially resveratrol analogs, in this research, the basic stilbene skeleton was used as a structural unit for new carbamates designed as potentially highly selective butyrylcholinesterase (BChE) inhibitors with excellent absorption, distribution, metabolism, excretion and toxicity ADMET properties. The inhibitory activity of newly prepared carbamates - was tested toward the enzymes acetylcholinesterase (AChE) and BChE. In the tested group of compounds, the leading inhibitors were and , which achieved excellent selective inhibitory activity for BChE with IC values of 0.
View Article and Find Full Text PDFPharmacol Rep
January 2025
Department of Translational Neuroscience, Center for Addiction Research, Wake Forest University School of Medicine, 115 South Chestnut St, Winston-Salem, NC, 27101, USA.
Background: Cocaine Use Disorder (CUD) remains a significant problem in the United States, with high rates of relapse and no present FDA-approved treatment. The acetylcholine neurotransmitter system, specifically through modulation of muscarinic acetylcholine receptor (mAChR) function, has shown promise as a therapeutic target for multiple aspects of CUD. Enhancement of the M mAChR subtype via positive allosteric modulation has been shown to inhibit the behavioral and neurochemical effects of cocaine across several rodent models of CUD.
View Article and Find Full Text PDFJ Family Med Prim Care
December 2024
Medicines Evaluation Unit, Manchester University National Health Service Foundation Trust, University of Manchester, Manchester, United Kingdom.
Context: An inhaled corticosteroid (ICS) in combination with a long-acting β2-agonist (LABA) is a common treatment approach for asthma patients not controlled on ICS alone, but a significant proportion of patients remain uncontrolled on this combination and treatment adherence can also be a challenge. One of the options for adults whose asthma is uncontrolled in an ICS/LABA is the addition of a long-acting muscarinic receptor antagonist (LAMA), an approach commonly referred to as 'triple therapy'. The use of medium-strength ICS/LABA/LAMA is established in treating chronic obstructive pulmonary disease but is less well-established in asthma.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Integrative Science Center of Germplasm Creation in Western China (CHONGQING) Science City, SWU-TAAHC Medicinal Plant Joint R&D Centre, School of Life Sciences, Southwest University, Chongqing 400715, China.
is a medicinal plant and an important source for the commercial production of tropane alkaloids (TAs), such as scopolamine and hyoscyamine, which are used clinically for their anticholinergic properties. In this study, we identified 16 metallocarboxypeptidase inhibitor (MCPI) genes from (), which are grouped into three subgroups based on phylogenetic relationships and are distributed across 10 chromosomes. Promoter analysis showed that most elements were related to defense and stress responses, such as drought, low-temperature, ABA (abscisic acid), GA (gibberellin), auxin, light and MeJA responsiveness.
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