FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2896569934> ?p ?o ?g. }

• W2896569934 endingPage "808" @default.
• W2896569934 startingPage "799" @default.
• W2896569934 abstract "The lysergamide lysergic acid diethylamide (LSD) is a prototypical classical hallucinogen with remarkably high potency. LSD remains a popular recreational drug but is also becoming an important research tool for medical and neuroscience studies. Recently, several lysergamides that are close structural analogs of LSD have been sold as recreational drugs, which suggests that further studies are needed to explore the pharmacological properties of these compounds. In this present investigation, another LSD congener, N-ethyl-N-cyclopropyl lysergamide (ECPLA), which to date has not been marketed as a recreational substance, was evaluated for its pharmacological features relative to those previously reported for LSD. The experiments focused on interactions with the 5-HT2A receptor, which is responsible for mediating the psychedelic effects of LSD and other hallucinogens. Competitive binding assays were performed to measure the affinity of ECPLA for 27 monoamine receptors. The ability of ECPLA to activate human 5-HT2 receptor subtypes was assessed using calcium mobilization assays. Head twitch response (HTR) studies were conducted in C57BL/6J mice to determine whether ECPLA activates 5-HT2A receptors in vivo. Two other N-alkyl substituted lysergamides, N-methyl-N-isopropyl lysergamide (MIPLA) and N-methyl-N-propyl lysergamide (LAMPA), were also tested in the HTR paradigm for comparative purposes. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors. Additionally, ECPLA was found to be a potent, highly efficacious 5-HT2A agonist for Gq-mediated calcium flux. Treatment with ECPLA induced head twitches in mice with a median effective dose (ED50) of 317.2 nmol/kg (IP), which is ~ 40% of the potency observed previously for LSD. LAMPA (ED50 = 358.3 nmol/kg) was virtually equipotent with ECPLA in the HTR paradigm whereas MIPLA (ED50 = 421.7 nmol/kg) was slightly less potent than ECPLA. These findings demonstrate that the pharmacological properties of ECPLA, MIPLA, and LAMPA are reminiscent of LSD and other lysergamide hallucinogens." @default.
• W2896569934 created "2018-10-26" @default.
• W2896569934 creator A5005457342 @default.
• W2896569934 creator A5006602823 @default.
• W2896569934 creator A5011122453 @default.
• W2896569934 creator A5020790730 @default.
• W2896569934 creator A5036162393 @default.
• W2896569934 creator A5054411523 @default.
• W2896569934 creator A5059306266 @default.
• W2896569934 creator A5060931486 @default.
• W2896569934 date "2018-10-08" @default.
• W2896569934 modified "2023-09-27" @default.
• W2896569934 title "Pharmacological characterization of the LSD analog N-ethyl-N-cyclopropyl lysergamide (ECPLA)" @default.
• W2896569934 cites W1727963951 @default.
• W2896569934 cites W1897852281 @default.
• W2896569934 cites W1969178306 @default.
• W2896569934 cites W1974195654 @default.
• W2896569934 cites W1980453588 @default.
• W2896569934 cites W1997058647 @default.
• W2896569934 cites W2009134620 @default.
• W2896569934 cites W2014120139 @default.
• W2896569934 cites W2016210950 @default.
• W2896569934 cites W2019963944 @default.
• W2896569934 cites W2036961427 @default.
• W2896569934 cites W2052414519 @default.
• W2896569934 cites W2067481209 @default.
• W2896569934 cites W2074577073 @default.
• W2896569934 cites W2074631079 @default.
• W2896569934 cites W2078821747 @default.
• W2896569934 cites W2089084116 @default.
• W2896569934 cites W2091930672 @default.
• W2896569934 cites W2097186407 @default.
• W2896569934 cites W2107095581 @default.
• W2896569934 cites W2109884356 @default.
• W2896569934 cites W2120981694 @default.
• W2896569934 cites W2146585068 @default.
• W2896569934 cites W2147962956 @default.
• W2896569934 cites W2164276826 @default.
• W2896569934 cites W2170848267 @default.
• W2896569934 cites W2256008574 @default.
• W2896569934 cites W2266766602 @default.
• W2896569934 cites W2275444639 @default.
• W2896569934 cites W2306810735 @default.
• W2896569934 cites W2312324544 @default.
• W2896569934 cites W2336389811 @default.
• W2896569934 cites W2341558148 @default.
• W2896569934 cites W2413573456 @default.
• W2896569934 cites W2413713893 @default.
• W2896569934 cites W2419284308 @default.
• W2896569934 cites W2581696375 @default.
• W2896569934 cites W2582692487 @default.
• W2896569934 cites W2589071607 @default.
• W2896569934 cites W2603180085 @default.
• W2896569934 cites W2603746317 @default.
• W2896569934 cites W2604586582 @default.
• W2896569934 cites W2604795661 @default.
• W2896569934 cites W2621905925 @default.
• W2896569934 cites W2756069429 @default.
• W2896569934 cites W2760207472 @default.
• W2896569934 cites W2760291954 @default.
• W2896569934 cites W2761856500 @default.
• W2896569934 cites W2789608017 @default.
• W2896569934 cites W3165049600 @default.
• W2896569934 cites W2171275385 @default.
• W2896569934 doi "https://doi.org/10.1007/s00213-018-5055-9" @default.
• W2896569934 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6848745" @default.
• W2896569934 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30298278" @default.
• W2896569934 hasPublicationYear "2018" @default.
• W2896569934 type Work @default.
• W2896569934 sameAs 2896569934 @default.
• W2896569934 citedByCount "19" @default.
• W2896569934 countsByYear W28965699342019 @default.
• W2896569934 countsByYear W28965699342020 @default.
• W2896569934 countsByYear W28965699342021 @default.
• W2896569934 countsByYear W28965699342022 @default.
• W2896569934 countsByYear W28965699342023 @default.
• W2896569934 crossrefType "journal-article" @default.
• W2896569934 hasAuthorship W2896569934A5005457342 @default.
• W2896569934 hasAuthorship W2896569934A5006602823 @default.
• W2896569934 hasAuthorship W2896569934A5011122453 @default.
• W2896569934 hasAuthorship W2896569934A5020790730 @default.
• W2896569934 hasAuthorship W2896569934A5036162393 @default.
• W2896569934 hasAuthorship W2896569934A5054411523 @default.
• W2896569934 hasAuthorship W2896569934A5059306266 @default.
• W2896569934 hasAuthorship W2896569934A5060931486 @default.
• W2896569934 hasBestOaLocation W28965699342 @default.
• W2896569934 hasConcept C124315065 @default.
• W2896569934 hasConcept C170493617 @default.
• W2896569934 hasConcept C185592680 @default.
• W2896569934 hasConcept C2775864247 @default.
• W2896569934 hasConcept C2776125444 @default.
• W2896569934 hasConcept C2778938600 @default.
• W2896569934 hasConcept C2779871769 @default.
• W2896569934 hasConcept C55493867 @default.
• W2896569934 hasConcept C71924100 @default.
• W2896569934 hasConcept C98274493 @default.
• W2896569934 hasConceptScore W2896569934C124315065 @default.
• W2896569934 hasConceptScore W2896569934C170493617 @default.

• next