Bispyridinium oximes with one (K865, K866, K867) or two (K868, K869, K870) ortho-positioned chlorine moiety, analogous to previously known K027, K048 and K203 oximes, and potent reactivators of human acetylcholinesterase (AChE) inhibited by nerve agents, were tested in the reactivation of human butyrylcholinesterase (BChE) inhibited by sarin, cyclosarin, VX, and tabun. A previously highlighted AChE reactivator, dichlorinated bispyridinium oxime with propyl linker (K868), was tested in more detail for reactivation of four nerve agent-BChE conjugates. Its BChE reactivation potency was showed to be promising when compared to the standard oximes used in medical practice, asoxime (HI-6) and pralidoxime (2-PAM), especially in case of sarin and tabun. This finding could be used in the pseudo-catalytic scavenging of the most nerve agents due to its cumulative capacity to reactivate both AChE and BChE.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.cbi.2019.04.020DOI Listing

Publication Analysis

Top Keywords

nerve agents
12
inhibited nerve
8
butyrylcholinesterase inhibited
4
nerve
4
agents efficiently
4
efficiently reactivated
4
reactivated chlorinated
4
chlorinated pyridinium
4
oximes
4
pyridinium oximes
4

Similar Publications

Postpartum pyogenic sacroiliitis masquerading as sciatic neuropathy.

BMJ Case Rep

January 2025

Department of Orthopedics, SDM College of Medical Sciences and Hospital, Shri Dharmasthala Manjunatheshwara University, Dharwad, Karnataka, India.

Low back pain is common in women, especially during pregnancy and puerperium. Septic sacroiliitis, a rare cause of back pain in the postpartum period can mimic other common causes of low back pain like muscle strain, urinary tract infection, pelvic inflammatory disease, endometritis and intervertebral disc prolapse. The proximity of the sacroiliac joint to the sacral nerve plexus results in septic sacroiliitis frequently presenting with symptoms mimicking intervertebral disc prolapse.

View Article and Find Full Text PDF

Metformin ameliorates peripheral neuropathy in diabetic rats by downregulating autophagy via the AMPK pathway.

Arch Endocrinol Metab

January 2025

Fuzhou First General Hospital Affiliated with Fujian Medical University Department of Endocrinology FuzhouFujian China Department of Endocrinology, Fuzhou First General Hospital Affiliated with Fujian Medical University, Fuzhou, Fujian, China.

Objective: Diabetic neuropathy (DN) is an important complication of diabetes mellitus. Autophagy is considered to be potentially involved in the regulation of DN. Metformin is broadly utilized in the first-line treatment of diabetes.

View Article and Find Full Text PDF

Background: Parkinson's disease (PD) is a neurodegenerative disorder characterized by protein aggregates mostly consisting of misfolded alpha-synuclein (αSyn). Progressive degeneration of midbrain dopaminergic neurons (mDANs) and nigrostriatal projections results in severe motor symptoms. While the preferential loss of mDANs has not been fully understood yet, the cell type-specific vulnerability has been linked to a unique intracellular milieu, influenced by dopamine metabolism, high demand for mitochondrial activity, and increased level of oxidative stress (OS).

View Article and Find Full Text PDF

Aim: The objective of the present study is to assess and compare the effectiveness of two different anesthetic agents, namely, 4% articaine and 2% lignocaine, in the extraction of primary molar teeth in children.

Materials And Methods: The study included 25 children requiring bilateral extractions of primary molar, with extraction performed on one side with 4% articaine and the contralateral side extraction with 2% lignocaine at two separate appointments. The anesthetic efficacy was evaluated objectively by assessing pain and the child's behavior at baseline, during injection and during extraction using the sound, eye, and motor (SEM) scale objectively, and subjectively using the faces pain rating scale (FPS).

View Article and Find Full Text PDF

Background: Multiple sclerosis (MS) is a chronic autoimmune condition that damages the myelin sheath of neurons in the central nervous system, resulting in compromised nerve transmission and motor impairment. The astrocytopathy is considered one of the prominent etiological factor in the pathophysiology of demyelination in MS. The expression level of ceramide synthase-2 (CS-2) is yet to be established in the pathophysiology of astrocytopathy although the derailed ceramide biosynthetic pathways is well demonstrated in the pathophysiology of demyelination.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!