Agonist Antagonist Interactions at the Rapidly Desensitizing P2X3 Receptor
نویسندگان
چکیده
منابع مشابه
Agonist Antagonist Interactions at the Rapidly Desensitizing P2X3 Receptor
P2X3 receptors (P2XRs), as members of the purine receptor family, are deeply involved in chronic pain sensation and therefore, specific, competitive antagonists are of great interest for perspective pain management. Heretofore, Schild plot analysis has been commonly used for studying the interaction of competitive antagonists and the corresponding receptor. Unfortunately, the steady-state betwe...
متن کاملThe effect of intracerebroventricular administration of CCK receptor agonist and antagonist in nerve-Iigated mice
In the present study the effect of intracerebroventricular (ICV) injection of cerulein, an agonist of CCK receptor and proglumide, a receptor antagonist for hyperalgesia induced by sciatic nerve ligation were investigated in mice. Subcutaneous administration of morphine caused anti-nociception in both intact and nerve-ligated mice. However, the response to opioids was lower in ligated mice as c...
متن کاملDesensitizing interactions
of receptor desensitization. Mutations that strengthen this interaction are more resistant to desensitization, whereas disruption of dimerization promotes desensitization. Dimer interaction takes place between domain 1 of the ligand-binding core in each subunit. When these interactions are strong, These studies also explain the mode of action of a drug that promotes AMPA activation, cyclothiazi...
متن کاملNew insights into interactions between the human PTH/PTHrP receptor and agonist/antagonist binding.
We prepared a polyclonal antiserum [Ab-(88-97)] against residues 88-97 of the NH2-terminal tail of the human (h) parathyroid hormone (PTH)/PTH-related protein (PTHrP) receptor. Ab-(88-97) bound specifically to the receptor, as assessed by fluorescence-activated cell sorter analysis of HEK C21 cells, which stably express ∼400,000 hPTH/PTHrP receptors per cell. Unlike PTH, Ab-(88-97) binding did ...
متن کاملATP, an agonist at the rat P2Y(4) receptor, is an antagonist at the human P2Y(4) receptor.
The nucleotide selectivities of the human P2Y(4) (hP2Y(4)) and rat P2Y(4) (rP2Y(4)) receptor stably expressed in 1321N1 human astrocytoma cells were determined by measuring increases in intracellular [Ca(2+)] under conditions that minimized metabolism, bioconversion, and endogenous nucleotide release. In cells expressing the hP2Y(4) receptor, UTP, GTP, and ITP all increased intracellular [Ca(2+...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: PLoS ONE
سال: 2013
ISSN: 1932-6203
DOI: 10.1371/journal.pone.0079213