Probe dependence of allosteric enhancers on the binding affinity of adenosine A1‐receptor agonists at rat and human A1‐receptors measured using NanoBRET

Cooper, Samantha L.; Soave, Mark; Jörg, Manuela; Scammells, Peter J.; Woolard, Jeanette; Hill, Stephen J.

doi:10.1111/bph.14575

All Outputs (8)

Role of endothelin ETA receptors in the hypertension induced by the VEGFR-2 kinase inhibitors axitinib and lenvatinib in conscious freely-moving rats (2023)
Journal Article

Receptor tyrosine kinase inhibitors (RTKIs) suppress tumour growth by targeting vascular endothelial growth factor receptor 2 (VEGFR-2) which is an important mediator of angiogenesis. Here, we demonstrate that two potent RTKIs, axitinib and lenvatini... Read More about Role of endothelin ETA receptors in the hypertension induced by the VEGFR-2 kinase inhibitors axitinib and lenvatinib in conscious freely-moving rats.

COVID-19-Induced Myocarditis: Pathophysiological Roles of ACE2 and Toll-like Receptors (2023)
Journal Article

The clinical manifestations of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection responsible for coronavirus disease 2019 (COVID-19) commonly include dyspnoea and fatigue, and they primarily involve the lungs. However, extra-... Read More about COVID-19-Induced Myocarditis: Pathophysiological Roles of ACE2 and Toll-like Receptors.

Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists (2022)
Journal Article

A2A and A2B adenosine receptors produce regionally selective regulation of vascular tone and elicit differing effects on mean arterial pressure (MAP), whilst inducing tachycardia. The tachycardia induced by the stimulation of A2A or A2B receptors has... Read More about Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists.

Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation (2022)
Journal Article

Adenosine is a local mediator that regulates changes in the cardiovascular system via activation of four G protein-coupled receptors (A1, A2A, A2B, A3). Here, we have investigated the effect of A2A and A2B-selective agonists on vasodilatation in thre... Read More about Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation.

Monitoring haemodynamic changes in rodent models to better inform safety pharmacology: Novel insights from in vivo studies and waveform analysis (2022)
Journal Article

Animal models are essential for assessing cardiovascular responses to novel therapeutics. Cardiovascular safety liabilities represent a leading cause of drug attrition and better preclinical measurements are essential to predict drug-related toxiciti... Read More about Monitoring haemodynamic changes in rodent models to better inform safety pharmacology: Novel insights from in vivo studies and waveform analysis.

Role of the renin–angiotensin–aldosterone and kinin–kallikrein systems in the cardiovascular complications of COVID-19 and long COVID (2021)
Journal Article

Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) is the virus responsible for the COVID-19 pandemic. Patients may present as asymptomatic or demonstrate mild to severe and life-threatening symptoms. Although COVID-19 has a respiratory foc... Read More about Role of the renin–angiotensin–aldosterone and kinin–kallikrein systems in the cardiovascular complications of COVID-19 and long COVID.

Long‐term cardiovascular effects of vandetanib and pazopanib in normotensive rats (2019)
Journal Article

Vandetanib and pazopanib are clinically available, multi‐targeted inhibitors of vascular endothelial growth factor (VEGF) and platelet‐derived growth factor (PDGF) receptor tyrosine kinases. Short‐term VEGF receptor inhibition is associated with hype... Read More about Long‐term cardiovascular effects of vandetanib and pazopanib in normotensive rats.

Probe dependence of allosteric enhancers on the binding affinity of adenosine A1‐receptor agonists at rat and human A1‐receptors measured using NanoBRET (2019)
Journal Article

Background and Purpose: Adenosine is a local mediator that regulates a number of physiological and pathological processes via activation of adenosine A1‐receptors. The activity of adenosine can be regulated at the level of its target receptor via dru... Read More about Probe dependence of allosteric enhancers on the binding affinity of adenosine A1‐receptor agonists at rat and human A1‐receptors measured using NanoBRET.