FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3015097529> ?p ?o ?g. }

• W3015097529 endingPage "172918" @default.
• W3015097529 startingPage "172918" @default.
• W3015097529 abstract "Synthetic cannabinoid receptor agonists (SCRAs) possess high abuse liability and complex toxicological profiles, making them serious threats to public health. EG-018 is a SCRA that has been detected in both illicit products and human samples, but it has received little attention to date. The current studies investigated EG-018 at human CB1 and CB2 receptors expressed in HEK293 cells in [3H]CP55,940 competition binding, [35S]GTPγS binding and forskolin-stimulated cAMP production. EG-018 was also tested in vivo for its ability to produce cannabimimetic and abuse-related effects in the cannabinoid tetrad and THC drug discrimination, respectively. EG-018 exhibited high affinity at CB1 (21 nM) and at CB2 (7 nM), but in contrast to typical SCRAs, behaved as a weak partial agonist in [35S]GTPγS binding, exhibiting lower efficacy but greater potency, than that of THC at CB1 and similar potency and efficacy at CB2. EG-018 inhibited forskolin-stimulated cAMP with similar efficacy but lower potency, compared to THC, which was likely due to high receptor density facilitating saturation of this signaling pathway. In mice, EG-018 (100 mg/kg, 30 min) administered intraperitoneally (i.p.) did not produce effects in the tetrad or drug discrimination nor did it shift THC's ED50 value in drug discrimination when administered before THC, suggesting EG-018 has negligible occupancy of brain CB1 receptors following i.p. administration. Following intravenous (i.v.) administration, EG-018 (56 mg/kg) produced hypomotility, catalepsy, and hypothermia, but only catalepsy was blocked by the selective CB1 antagonist rimonabant (3 mg/kg, i.v.). Additional studies of EG-018 and its structural analogues could provide further insight into how cannabinoids exert efficacy through the cannabinoid receptors." @default.
• W3015097529 created "2020-04-10" @default.
• W3015097529 creator A5019318036 @default.
• W3015097529 creator A5022589029 @default.
• W3015097529 creator A5029174750 @default.
• W3015097529 creator A5029257596 @default.
• W3015097529 creator A5029415963 @default.
• W3015097529 creator A5029665394 @default.
• W3015097529 creator A5043291449 @default.
• W3015097529 creator A5052813563 @default.
• W3015097529 creator A5052855527 @default.
• W3015097529 creator A5077728218 @default.
• W3015097529 creator A5083280161 @default.
• W3015097529 date "2020-06-01" @default.
• W3015097529 modified "2023-10-17" @default.
• W3015097529 title "In vitro and in vivo pharmacological evaluation of the synthetic cannabinoid receptor agonist EG-018" @default.
• W3015097529 cites W100628994 @default.
• W3015097529 cites W1534915247 @default.
• W3015097529 cites W1542041788 @default.
• W3015097529 cites W1899851239 @default.
• W3015097529 cites W1965926793 @default.
• W3015097529 cites W1968629237 @default.
• W3015097529 cites W1976134052 @default.
• W3015097529 cites W1979668165 @default.
• W3015097529 cites W1987400624 @default.
• W3015097529 cites W1989096515 @default.
• W3015097529 cites W1989881153 @default.
• W3015097529 cites W2000046347 @default.
• W3015097529 cites W2006280591 @default.
• W3015097529 cites W2010284869 @default.
• W3015097529 cites W2017548821 @default.
• W3015097529 cites W2021294213 @default.
• W3015097529 cites W2021765490 @default.
• W3015097529 cites W2029505282 @default.
• W3015097529 cites W2032315023 @default.
• W3015097529 cites W2048921576 @default.
• W3015097529 cites W2069780284 @default.
• W3015097529 cites W2074141371 @default.
• W3015097529 cites W2079071356 @default.
• W3015097529 cites W2085052529 @default.
• W3015097529 cites W2085424227 @default.
• W3015097529 cites W2102479939 @default.
• W3015097529 cites W2104958800 @default.
• W3015097529 cites W2113475849 @default.
• W3015097529 cites W2117833691 @default.
• W3015097529 cites W2131204129 @default.
• W3015097529 cites W2135180673 @default.
• W3015097529 cites W2178564482 @default.
• W3015097529 cites W2306386326 @default.
• W3015097529 cites W2326889891 @default.
• W3015097529 cites W2334189569 @default.
• W3015097529 cites W2409706631 @default.
• W3015097529 cites W2417140329 @default.
• W3015097529 cites W2491075455 @default.
• W3015097529 cites W2512420186 @default.
• W3015097529 cites W2577536653 @default.
• W3015097529 cites W2593385402 @default.
• W3015097529 cites W2614187876 @default.
• W3015097529 cites W2619627104 @default.
• W3015097529 cites W2749177504 @default.
• W3015097529 cites W2793993257 @default.
• W3015097529 cites W2794293351 @default.
• W3015097529 cites W2800510547 @default.
• W3015097529 cites W2801605997 @default.
• W3015097529 cites W2892282544 @default.
• W3015097529 cites W2903891151 @default.
• W3015097529 cites W2926684005 @default.
• W3015097529 cites W2952038621 @default.
• W3015097529 cites W2970884997 @default.
• W3015097529 doi "https://doi.org/10.1016/j.pbb.2020.172918" @default.
• W3015097529 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7239729" @default.
• W3015097529 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32247816" @default.
• W3015097529 hasPublicationYear "2020" @default.
• W3015097529 type Work @default.
• W3015097529 sameAs 3015097529 @default.
• W3015097529 citedByCount "8" @default.
• W3015097529 countsByYear W30150975292021 @default.
• W3015097529 countsByYear W30150975292022 @default.
• W3015097529 countsByYear W30150975292023 @default.
• W3015097529 crossrefType "journal-article" @default.
• W3015097529 hasAuthorship W3015097529A5019318036 @default.
• W3015097529 hasAuthorship W3015097529A5022589029 @default.
• W3015097529 hasAuthorship W3015097529A5029174750 @default.
• W3015097529 hasAuthorship W3015097529A5029257596 @default.
• W3015097529 hasAuthorship W3015097529A5029415963 @default.
• W3015097529 hasAuthorship W3015097529A5029665394 @default.
• W3015097529 hasAuthorship W3015097529A5043291449 @default.
• W3015097529 hasAuthorship W3015097529A5052813563 @default.
• W3015097529 hasAuthorship W3015097529A5052855527 @default.
• W3015097529 hasAuthorship W3015097529A5077728218 @default.
• W3015097529 hasAuthorship W3015097529A5083280161 @default.
• W3015097529 hasBestOaLocation W30150975292 @default.
• W3015097529 hasConcept C126322002 @default.
• W3015097529 hasConcept C148001335 @default.
• W3015097529 hasConcept C170493617 @default.
• W3015097529 hasConcept C185592680 @default.
• W3015097529 hasConcept C202751555 @default.
• W3015097529 hasConcept C2778938600 @default.

• next