Carbetocin is a Functional Selective Gq Agonist That Does Not Promote Oxytocin Receptor Recycling After Inducing β‐Arrestin‐Independent Internalisation
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چکیده
منابع مشابه
Selexipag: a selective prostacyclin receptor agonist that does not affect rat gastric function.
Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide] is an orally available prostacyclin (PGI(2)) receptor (IP receptor) agonist that is chemically distinct from PGI(2) and is in clinical development for the treatment of pulmonary arterial hypertension. Selexipag is highly selective for the human IP receptor in vitro, whereas analogs of PGI(2) can act...
متن کاملJPET#169748 TITLE PAGE Selexipag: a selective prostacyclin receptor agonist that does not affect rat gastric function
word count: 250
متن کاملAn opioid agonist that does not induce mu-opioid receptor--arrestin interactions or receptor internalization.
G protein-coupled receptor desensitization and trafficking are important regulators of opioid receptor signaling that can dictate overall drug responsiveness in vivo. Furthermore, different mu-opioid receptor (muOR) ligands can lead to varying degrees of receptor regulation, presumably because of distinct structural conformations conferred by agonist binding. For example, morphine binding produ...
متن کاملAn Opioid Agonist that Does Not Induce -Opioid Receptor— Arrestin Interactions or Receptor Internalization
G protein-coupled receptor desensitization and trafficking are important regulators of opioid receptor signaling that can dictate overall drug responsiveness in vivo. Furthermore, different -opioid receptor ( OR) ligands can lead to varying degrees of receptor regulation, presumably because of distinct structural conformations conferred by agonist binding. For example, morphine binding produces...
متن کاملOxytocin and carbetocin effects on spontaneous behavior of male rats: modulation by oxytocin receptor antagonists.
OBJECTIVES Oxytocin (OXY) in addition to peripheral actions has many central regulatory functions which can be studied on animal models. In the present study we examined in rats, which behavioral actions of OXY and long-acting carba-analog of OXY carbetocin (CBT) in the open-field can be inhibited by OXY-receptor antagonists. Our interest focused on the behavioral patterns considered indicative...
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ژورنال
عنوان ژورنال: Journal of Neuroendocrinology
سال: 2016
ISSN: 0953-8194,1365-2826
DOI: 10.1111/jne.12363