FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W288293711> ?p ?o ?g. }

• W288293711 abstract "Opiates such as morphine are the choice analgesic in the treatment of chronic pain due to their potent and rapid action. Opioid receptors belong to the family of G protein-coupled receptors (GPCRs), one of the largest gene families in the mammalian genome. The OPRM1 gene encodes the mu opioid receptor, which is the primary site of action for morphine and other commonly used opioids such as heroin, fentanyl, and methadone. The long-term use of opiates is limited because of the development of tolerance and dependence, as well as respiratory suppression and constipation. Due to their clinical importance, various strategies have been considered for making opiates more effective while curbing liabilities such as addiction. One such strategy has been to use a combination of drugs to improve the effectiveness of morphine. In particular, delta opioid receptor (OPRD1) ligands have been useful in enhancing morphine’s potency, but the underlying molecular basis is not understood. It has been shown that modulation of receptor function by physical association between OPRM1 and OPRD1 is a potential mechanism; heteromerization of OPRM1 with OPRD1 leads to the modulation of receptor binding and signaling properties. It has further been shown that the selective activation of the OPRM1-OPRD1 heteromer by a combination of OPRM1 agonist with OPRD1 antagonist can be blocked by antibodies that selectively recognize the heteromer. Therefore, the identification of compounds that selectively activate OPRM1-OPRD1 heterodimerization may have potential in the treatment of pain and alleviate unwanted effects associated with opiate use. The Scripps Research Institute Molecular Screening Center (SRIMSC), part of the Molecular Libraries Probe Production Centers Network (MLPCN), reports here an agonist for OPRM1-OPRD1 heterdimerization, ML335, with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively." @default.
• W288293711 created "2016-06-24" @default.
• W288293711 creator A5001640688 @default.
• W288293711 creator A5003203423 @default.
• W288293711 creator A5006260657 @default.
• W288293711 creator A5019762035 @default.
• W288293711 creator A5021420487 @default.
• W288293711 creator A5025706653 @default.
• W288293711 creator A5030014468 @default.
• W288293711 creator A5036011720 @default.
• W288293711 creator A5042914450 @default.
• W288293711 creator A5053630827 @default.
• W288293711 creator A5077665475 @default.
• W288293711 creator A5085356292 @default.
• W288293711 creator A5088494095 @default.
• W288293711 creator A5089826369 @default.
• W288293711 date "2013-04-05" @default.
• W288293711 modified "2023-09-23" @default.
• W288293711 title "Characterization of an agonist probe for opioid receptor mu 1 (OPRM1)-opioid receptor delta 1 (OPRD1) heterodimerization" @default.
• W288293711 cites W1562458137 @default.
• W288293711 cites W1603898092 @default.
• W288293711 cites W1918768783 @default.
• W288293711 cites W1967259165 @default.
• W288293711 cites W1968179127 @default.
• W288293711 cites W1970100138 @default.
• W288293711 cites W1974354099 @default.
• W288293711 cites W1977877988 @default.
• W288293711 cites W1979179968 @default.
• W288293711 cites W1980325059 @default.
• W288293711 cites W1982525225 @default.
• W288293711 cites W1982650478 @default.
• W288293711 cites W1990038772 @default.
• W288293711 cites W1991965941 @default.
• W288293711 cites W1996075048 @default.
• W288293711 cites W2004519217 @default.
• W288293711 cites W2004800999 @default.
• W288293711 cites W2005418171 @default.
• W288293711 cites W2005699747 @default.
• W288293711 cites W2010694257 @default.
• W288293711 cites W2010993054 @default.
• W288293711 cites W2014306255 @default.
• W288293711 cites W2016989363 @default.
• W288293711 cites W2017212166 @default.
• W288293711 cites W2023364037 @default.
• W288293711 cites W2036104418 @default.
• W288293711 cites W2038011107 @default.
• W288293711 cites W2045669714 @default.
• W288293711 cites W2047063796 @default.
• W288293711 cites W2047308059 @default.
• W288293711 cites W2048134537 @default.
• W288293711 cites W2049559865 @default.
• W288293711 cites W2051526283 @default.
• W288293711 cites W2056301613 @default.
• W288293711 cites W2057896776 @default.
• W288293711 cites W2057910472 @default.
• W288293711 cites W2059961278 @default.
• W288293711 cites W2060793088 @default.
• W288293711 cites W2062141191 @default.
• W288293711 cites W2069685762 @default.
• W288293711 cites W2070324798 @default.
• W288293711 cites W2078585784 @default.
• W288293711 cites W2085948860 @default.
• W288293711 cites W2088974390 @default.
• W288293711 cites W2092905357 @default.
• W288293711 cites W2097957649 @default.
• W288293711 cites W2114163388 @default.
• W288293711 cites W2128338277 @default.
• W288293711 cites W2137246832 @default.
• W288293711 cites W2153537996 @default.
• W288293711 cites W2159254316 @default.
• W288293711 cites W2161083956 @default.
• W288293711 cites W2163652380 @default.
• W288293711 cites W2163824404 @default.
• W288293711 cites W2165431421 @default.
• W288293711 cites W2167212772 @default.
• W288293711 cites W2172146299 @default.
• W288293711 cites W2312227080 @default.
• W288293711 cites W3144946601 @default.
• W288293711 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23833799" @default.
• W288293711 hasPublicationYear "2013" @default.
• W288293711 type Work @default.
• W288293711 sameAs 288293711 @default.
• W288293711 citedByCount "0" @default.
• W288293711 crossrefType "journal-article" @default.
• W288293711 hasAuthorship W288293711A5001640688 @default.
• W288293711 hasAuthorship W288293711A5003203423 @default.
• W288293711 hasAuthorship W288293711A5006260657 @default.
• W288293711 hasAuthorship W288293711A5019762035 @default.
• W288293711 hasAuthorship W288293711A5021420487 @default.
• W288293711 hasAuthorship W288293711A5025706653 @default.
• W288293711 hasAuthorship W288293711A5030014468 @default.
• W288293711 hasAuthorship W288293711A5036011720 @default.
• W288293711 hasAuthorship W288293711A5042914450 @default.
• W288293711 hasAuthorship W288293711A5053630827 @default.
• W288293711 hasAuthorship W288293711A5077665475 @default.
• W288293711 hasAuthorship W288293711A5085356292 @default.
• W288293711 hasAuthorship W288293711A5088494095 @default.
• W288293711 hasAuthorship W288293711A5089826369 @default.
• W288293711 hasConcept C135285700 @default.
• W288293711 hasConcept C141087196 @default.

• next