Matches in SemOpenAlex for { <https://semopenalex.org/work/W2092118947> ?p ?o ?g. }
- W2092118947 endingPage "56" @default.
- W2092118947 startingPage "41" @default.
- W2092118947 abstract "Enhanced sensitivity to noxious stimuli and the perception of non-noxious stimuli as painful are hallmark sensory perturbations associated with chronic pain. It is now appreciated that ATP, through its actions as an excitatory neurotransmitter, plays a prominent role in the initiation and maintenance of chronic pain states. Mechanistically, the ability of ATP to drive nociceptive sensitivity is mediated through direct interactions at neuronal P2X3 and P2X2/3 receptors. Extracellular ATP also activates P2X4, P2X7, and several P2Y receptors on glial cells within the spinal cord, which leads to a heightened state of neural-glial cell interaction in ongoing pain states. Following the molecular identification of the P2 receptor superfamilies, selective small molecule antagonists for several P2 receptor subtypes were identified, which have been useful for investigating the role of specific P2X receptors in preclinical chronic pain models. More recently, several P2X receptor antagonists have advanced into clinical trials for inflammation and pain. The development of orally bioavailable blockers for ion channels, including the P2X receptors, has been traditionally difficult due to the necessity of combining requirements for target potency and selectivity with suitable absorption distribution, metabolism, and elimination properties. Recent studies on the physicochemical properties of marketed orally bioavailable drugs, have identified several parameters that appear critical for increasing the probability of achieving suitable bioavailability, central nervous system exposure, and acceptable safety necessary for clinical efficacy. This review provides an overview of the antinociceptive pharmacology of P2X receptor antagonists and the chemical diversity and drug-like properties for emerging antagonists of P2X3, P2X2/3, P2X4, and P2X7 receptors." @default.
- W2092118947 created "2016-06-24" @default.
- W2092118947 creator A5062211075 @default.
- W2092118947 creator A5067147097 @default.
- W2092118947 creator A5073616909 @default.
- W2092118947 date "2011-11-16" @default.
- W2092118947 modified "2023-10-14" @default.
- W2092118947 title "P2X receptor antagonists for pain management: examination of binding and physicochemical properties" @default.
- W2092118947 cites W134994456 @default.
- W2092118947 cites W1499625036 @default.
- W2092118947 cites W1680053970 @default.
- W2092118947 cites W1773597617 @default.
- W2092118947 cites W1824528611 @default.
- W2092118947 cites W1897243328 @default.
- W2092118947 cites W1953611243 @default.
- W2092118947 cites W1964381081 @default.
- W2092118947 cites W1964855129 @default.
- W2092118947 cites W1966422137 @default.
- W2092118947 cites W1971513938 @default.
- W2092118947 cites W1972821149 @default.
- W2092118947 cites W1978269241 @default.
- W2092118947 cites W1979359788 @default.
- W2092118947 cites W1983504852 @default.
- W2092118947 cites W1988137843 @default.
- W2092118947 cites W1988889092 @default.
- W2092118947 cites W1989511196 @default.
- W2092118947 cites W1990063735 @default.
- W2092118947 cites W1995622771 @default.
- W2092118947 cites W1997982516 @default.
- W2092118947 cites W2000720249 @default.
- W2092118947 cites W2008312146 @default.
- W2092118947 cites W2014203427 @default.
- W2092118947 cites W2014683303 @default.
- W2092118947 cites W2015395924 @default.
- W2092118947 cites W2016575780 @default.
- W2092118947 cites W2023292963 @default.
- W2092118947 cites W2024608254 @default.
- W2092118947 cites W2027961128 @default.
- W2092118947 cites W2027981901 @default.
- W2092118947 cites W2030215451 @default.
- W2092118947 cites W2031434196 @default.
- W2092118947 cites W2032353075 @default.
- W2092118947 cites W2033498682 @default.
- W2092118947 cites W2034182613 @default.
- W2092118947 cites W2040066247 @default.
- W2092118947 cites W2042721486 @default.
- W2092118947 cites W2046824632 @default.
- W2092118947 cites W2047429147 @default.
- W2092118947 cites W2050181320 @default.
- W2092118947 cites W2054732161 @default.
- W2092118947 cites W2054829858 @default.
- W2092118947 cites W2056123178 @default.
- W2092118947 cites W2056148352 @default.
- W2092118947 cites W2059391185 @default.
- W2092118947 cites W2059490337 @default.
- W2092118947 cites W2062458432 @default.
- W2092118947 cites W2063255933 @default.
- W2092118947 cites W2063781307 @default.
- W2092118947 cites W2065686546 @default.
- W2092118947 cites W2065950517 @default.
- W2092118947 cites W2066320999 @default.
- W2092118947 cites W2069799943 @default.
- W2092118947 cites W2071674361 @default.
- W2092118947 cites W2074847975 @default.
- W2092118947 cites W2075715972 @default.
- W2092118947 cites W2076955704 @default.
- W2092118947 cites W2077549864 @default.
- W2092118947 cites W2078435077 @default.
- W2092118947 cites W2080060433 @default.
- W2092118947 cites W2080262910 @default.
- W2092118947 cites W2080603742 @default.
- W2092118947 cites W2081180556 @default.
- W2092118947 cites W2082547190 @default.
- W2092118947 cites W2090227348 @default.
- W2092118947 cites W2099163813 @default.
- W2092118947 cites W2104986316 @default.
- W2092118947 cites W2106753138 @default.
- W2092118947 cites W2111178472 @default.
- W2092118947 cites W2116230226 @default.
- W2092118947 cites W2116847572 @default.
- W2092118947 cites W2128994172 @default.
- W2092118947 cites W2131305615 @default.
- W2092118947 cites W2135732933 @default.
- W2092118947 cites W2140161110 @default.
- W2092118947 cites W2145280844 @default.
- W2092118947 cites W2149365742 @default.
- W2092118947 cites W2150904116 @default.
- W2092118947 cites W2156346381 @default.
- W2092118947 cites W2165271332 @default.
- W2092118947 cites W2170816637 @default.
- W2092118947 cites W2573095167 @default.
- W2092118947 doi "https://doi.org/10.1007/s11302-011-9272-5" @default.
- W2092118947 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3265705" @default.
- W2092118947 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22086553" @default.
- W2092118947 hasPublicationYear "2011" @default.
- W2092118947 type Work @default.
- W2092118947 sameAs 2092118947 @default.
- W2092118947 citedByCount "61" @default.