Biginelli dihydropyrimidines and their acetylated derivatives as L‐/T‐type calcium channel blockers: Synthesis, enantioseparation, and molecular modeling studies
Sign Up to like & getrecommendations! Published in 2025 at "Archiv Der Pharmazie"
DOI: 10.1002/ardp.202400584
Abstract: Biginelli dihydropyrimidines (DHPMs) are considered superior over 1,4‐dihydropyridines (DHPs) in terms of both light and metabolic stabilities. Nevertheless, DHPs dominate the market as the most prescribed calcium channel blockers with strong therapeutic potential in managing… read more here.
Keywords: calcium channel; biginelli dihydropyrimidines; channel blockers; calcium ... See more keywords
Translational Pharmacology of PRAX‐944, a Novel T‐Type Calcium Channel Blocker in Development for the Treatment of Essential Tremor
Sign Up to like & getrecommendations! Published in 2022 at "Movement Disorders"
DOI: 10.1002/mds.28969
Abstract: Essential tremor is the most common movement disorder with clear unmet need. Mounting evidence indicates tremor is caused by increased neuronal burst firing and oscillations in cerebello‐thalamo‐cortical circuitry and may be dependent on T‐type calcium… read more here.
Keywords: pharmacology; type calcium; essential tremor; channel ... See more keywords
Stimulation of L‐type calcium channels increases tyrosine hydroxylase and dopamine in ventral midbrain cells induced from somatic cells
Sign Up to like & getrecommendations! Published in 2020 at "Stem Cells Translational Medicine"
DOI: 10.1002/sctm.18-0180
Abstract: Making high‐quality dopamine (DA)‐producing cells for basic biological or small molecule screening studies is critical for the development of novel therapeutics for disorders of the ventral midbrain. Currently, many ventral midbrain assays have low signal‐to‐noise… read more here.
Keywords: type calcium; ventral midbrain; calcium; tyrosine hydroxylase ... See more keywords
L-type calcium channel blockers and a symptom complex mimicking de Melo-Souza’s syndrome
Sign Up to like & getrecommendations! Published in 2018 at "Neurological Sciences"
DOI: 10.1007/s10072-018-3662-1
Abstract: Dear Editor, Drugs are an important cause of tremor in the elderly and the second most common cause of Parkinsonism. Common medications which induce tremor include salbutamol, theophylline, valproate, anti-depressants, anti-psychotics, and anti-dopaminergics [1, 2].… read more here.
Keywords: calcium channel; melo souza; type calcium; channel blockers ... See more keywords
T-type calcium channels regulate medulloblastoma and can be targeted for therapy
Sign Up to like & getrecommendations! Published in 2025 at "Journal of Neuro-Oncology"
DOI: 10.1007/s11060-025-04967-5
Abstract: The goal of this study was to investigate the role and therapeutic targeting of T-type calcium channels in medulloblastoma, a common and deadly pediatric brain tumor that arises in the cerebellum. T-type calcium channel expression… read more here.
Keywords: calcium; cell; type calcium; expression ... See more keywords
Isoliensinine Eliminates Afterdepolarizations Through Inhibiting Late Sodium Current and L-Type Calcium Current
Sign Up to like & getrecommendations! Published in 2020 at "Cardiovascular Toxicology"
DOI: 10.1007/s12012-020-09597-z
Abstract: Isoliensinine (IL) extracted from lotus seed has a good therapeutic effect on cardiovascular diseases. However, its effect on ion channels of ventricular myocytes is still unclear. We used whole-cell patch-clamp techniques to detect the effects… read more here.
Keywords: late sodium; sodium current; calcium current; type calcium ... See more keywords
Discovery of Michael acceptor containing 1,4-dihydropyridines as first covalent inhibitors of L-/T-type calcium channels.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103187
Abstract: 1,4-Dihydropyridines (DHPs) are an important class of blockers targeting different calcium channel subtypes and have great therapeutic value against cardiovascular and neurophysiologic conditions. Here, we present the design of DHP-based hexahydroquinoline derivatives as either selective… read more here.
Keywords: covalent inhibitors; calcium channels; type calcium; michael acceptor ... See more keywords
Hydrogen sulfide inhibited L-type calcium channels (CaV1.2) via up-regulation of the channel sulfhydration in vascular smooth muscle cells.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2019.172455
Abstract: Hydrogen sulfide (H2S) exerts different effects on the cardiovascular system by modulating ion channels. The present study was to ascertain whether H2S affects L-type calcium (Ca2+) channels in vascular smooth muscle cells (VSMCs) and the… read more here.
Keywords: type calcium; vascular smooth; ca2; hydrogen sulfide ... See more keywords
Analysis of tetrodotoxin-sensitive sodium and low voltage-activated calcium channels in developing mouse retinal horizontal cells.
Sign Up to like & getrecommendations! Published in 2020 at "Experimental eye research"
DOI: 10.1016/j.exer.2020.108028
Abstract: Expression patterns of voltage-gated ion channels determine the spatio-temporal dynamics of ion currents that supply excitable neurons in developing tissue with proper electrophysiological properties. The purpose of the study was to identify fast cationic inward… read more here.
Keywords: voltage; sensitive sodium; calcium channels; type calcium ... See more keywords
Sociability impairments in Genetic Absence Epilepsy Rats from Strasbourg: Reversal by the T-type calcium channel antagonist Z944
Sign Up to like & getrecommendations! Published in 2017 at "Experimental Neurology"
DOI: 10.1016/j.expneurol.2017.06.022
Abstract: &NA; Childhood absence epilepsy (CAE) is associated with interictal co‐morbid symptoms including abnormalities in social behaviour. Genetic Absence Epilepsy Rats from Strasbourg (GAERS) is a model of CAE that exhibits physiological and behavioural alterations characteristic… read more here.
Keywords: z944; sociability; calcium channel; type calcium ... See more keywords
Calcitriol (1,25-dihydroxyvitamin D3) increases L-type calcium current via protein kinase A signaling and modulates calcium cycling and contractility in isolated mouse ventricular myocytes.
Sign Up to like & getrecommendations! Published in 2017 at "Heart rhythm"
DOI: 10.1016/j.hrthm.2016.12.013
Abstract: BACKGROUND Calcitriol, the bioactive metabolite of vitamin D, exerts its effects through interaction with the nuclear vitamin D receptor (VDR) to induce genomic responses. Calcitriol may also induce rapid responses via plasma membrane-associated VDR, involving… read more here.
Keywords: ca2 transients; type calcium; mouse ventricular; calcitriol ... See more keywords