Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]
, 2007 G protein–coupled receptors (GPCRs) exist in multiple dynamic states (e.g., ligand-bound, inactive, G protein–coupled) that influence G protein activation and ultimately response generation. In quantitative models of GPCR signaling that incorporate these
Kinzer-Ursem, Tamara L. +1 more
core +3 more sources
Dexmedetomidine: present and future directions [PDF]
Korean Journal of Anesthesiology, 2019 Dexmedetomidine is a potent, highly selective α-2 adrenoceptor agonist, with sedative, analgesic, anxiolytic, sympatholytic, and opioid-sparing properties.
Seongheon Lee
doaj +1 more source
A selective alpha1D-adrenoreceptor antagonist inhibits human prostate cancer cell proliferation and motility "in vitro" [PDF]
, 2016 The progression of prostate cancer (PC) to a metastatic hormone refractory disease is the major contributor to the overall cancer mortality in men, mainly because the conventional therapies are generally ineffective at this stage. Thus, other therapeutic
Bolchi, Cristiano +8 more
core +2 more sources
Indian Journal of Ophthalmology, 2015 Aim: To determine the effect of alpha-2-agonist (AA) premedication (PM) on intraocular pressure (IOP) following selective laser trabeculoplasty (SLT).
Julius T Oatts +2 more
doaj +1 more source
Histamine stimulates the proliferation of small and large cholangiocytes by activation of both IP3/Ca2+ and cAMP-dependent signaling mechanisms [PDF]
, 2012 Although large cholangiocytes exert their functions by activation of cyclic adenosine 3',5'-monophosphate (cAMP), Ca(2+)-dependent signaling regulates the function of small cholangiocytes. Histamine interacts with four receptors, H1-H4HRs.
Fanyin Meng +15 more
core +1 more source
Functional selectivity of GPCR-directed drug action through location bias. [PDF]
, 2017 G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco +6 more
core +3 more sources
Adjuvant pharmacological strategies for the musculoskeletal system during long‐term space missions
British Journal of Clinical Pharmacology, EarlyView., 2023 Abstract Despite 2 h of daily exercise training, muscle wasting and bone loss are still present after 6‐month missions to the international space station. Some crew members lose bone much faster than others. In preparation for missions to the Moon and Mars, space agencies are therefore reviewing their countermeasure portfolios.
Friederike Thomasius +2 more
wiley +1 more source
Spinal anesthesia for elective ceasarean section: use of different doses of hyperbaric bupivacaine associated with morphine and clonidine [PDF]
Acta Cirúrgica Brasileira, 2013 PURPOSE: To comparatively study the efficacy and maternal and fetal side-effects of two doses of bupivacaine associated with morphine and clonidine, administered by the subarachnoid route for cesarean section.
Angélica de Fátima de Assunção Braga +4 more
doaj +3 more sources
iScience, 2018 Summary: Adrenergic stimulation of brown adipose tissue (BAT) induces acute and long-term responses. The acute adrenergic response activates thermogenesis by uncoupling oxidative phosphorylation and enabling increased substrate oxidation.
Erin L. Brown +9 more
doaj +1 more source
Oral Administration of Levo-Tetrahydropalmatine Attenuates Reinstatement of Extinguished Cocaine Seeking by Cocaine, Stress or Drug-Associated Cues in Rats [PDF]
, 2011 Cocaine addiction is characterized by a persistently heightened susceptibility to drug relapse. For this reason, the identification of medications that prevent drug relapse is a critical goal of drug abuse research.
Baker, David A. +9 more
core +2 more sources