Results 101 to 110 of about 2,143 (224)

G protein‐coupled receptor‐mediated autophagy in health and disease

open access: yesBritish Journal of Pharmacology, EarlyView.
G protein‐coupled receptors (GPCRs) constitute the largest and most diverse superfamily of mammalian transmembrane proteins. These receptors are involved in a wide range of physiological functions and are targets for more than a third of available drugs in the market. Autophagy is a cellular process involved in degrading damaged proteins and organelles
Devrim Öz‐Arslan   +2 more
wiley   +1 more source

Novel FKBP prolyl isomerase 1A (FKBP12) ligand promotes functional improvement in SOD1G93A amyotrophic lateral sclerosis (ALS) mice

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Amyotrophic lateral sclerosis (ALS) is a devastating neurodegenerative disease with limited treatment options. ALS pathogenesis involves intricate processes within motor neurons, characterized by dysregulated Ca2+ influx and buffering in early ALS‐affected motor neurones. This study proposes the modulation of ryanodine receptors (
Laura Moreno‐Martinez   +17 more
wiley   +1 more source

Channel blocking properties of a series of nicotinic cholinergic agonists

open access: yesBiophysical Journal, 1993
Inhibition of the nicotinic acetylcholine receptor (nAChR) by channel blockade has been demonstrated with a variety of large organic cations, including several nicotinic agonists. We have studied the kinetics of channel blocking of a series of agonists which vary systematically in size and hydrophobicity due to a hydrocarbon chain from one to six ...
Robert E. Oswald, Alison A. Carter
openaire   +3 more sources

Oral hyoscine butylbromide exerts spasmolytic effects in both gastrointestinal and urogenital tissues in rats

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Hyoscine butylbromide (HBB) has a low oral (PO) bioavailability. Further, limited data on its activity on non‐gastrointestinal (GI) smooth muscle spasms after oral dosing are available, causing its effects beyond the GI tract to be questioned.
Sara Traserra   +4 more
wiley   +1 more source

Association of nicotinic acetylcholine receptors with central respiratory control in isolated brainstem-spinal cord preparation of neonatal rats

open access: yesBiological Research, 2006
Nicotine exposure is a risk factor in several breathing disorders Nicotinic acetylcholine receptors (nAChRs) exist in the ventrolateral medulla, an important site for respiratory control.
EIKI HATORI   +7 more
doaj  

Conformational dynamics of a nicotinic receptor neurotransmitter site

open access: yeseLife
Agonists enhance receptor activity by providing net-favorable binding energy to active over resting conformations, with efficiency (η) linking binding energy to gating.
Mrityunjay Singh   +4 more
doaj   +1 more source

Agonist-Antagonist Pouch Motors: Bidirectional Soft Actuators Enhanced by Thermally Responsive Peltier Elements [PDF]

open access: yes
In this study, we introduce a novel Mylar-based pouch motor design that leverages the reversible actuation capabilities of Peltier junctions to enable agonist-antagonist muscle mimicry in soft robotics. Addressing the limitations of traditional silicone-based materials, such as leakage and phase-change fluid degradation, our pouch motors filled with ...
arxiv   +1 more source

Role of nicotine receptor partial agonists in tobacco cessation

open access: yesIndian Journal of Psychiatry, 2014
One in three adults in India uses tobacco, a highly addictive substance in one or other form. In addition to prevention of tobacco use, offering evidence-based cessation services to dependent tobacco users constitutes an important approach in addressing this serious public health problem.
Pratima Murthy   +2 more
openaire   +3 more sources

ESG‐1‐60 and ESG‐1‐61: Novel dopamine D3 receptor‐preferring partial agonists/antagonists that inhibit cocaine taking and seeking in rodents

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Preclinical studies suggest that highly selective dopamine D3 receptor (D3R) antagonists or partial agonists hold promise for treating substance use disorders. However, their limited effectiveness in reducing cocaine self‐administration is a major drawback.
Omar Soler‐Cedeño   +9 more
wiley   +1 more source

Epibatidine Induces Long-Term Potentiation (LTP) via Activation of α4β2 Nicotinic Acetylcholine Receptors (nAChRs) In Vivo in the Intact Mouse Dentate Gyrus: Both α7 and α4β2 nAChRs Essential to Nicotinic LTP

open access: yesJournal of Pharmacological Sciences, 2003
: Activation of nicotinic acetylcholine receptors (nAChRs) induces nocotinic long-term potentiation (LTPn) in vivo in the mouse dentate gyrus. We have found that α4β2 nAChRs activated by epibatidine induce LTPn, the full size of which requires the ...
Shogo Matsuyama, Akira Matsumoto
doaj  

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