Matches in SemOpenAlex for { <https://semopenalex.org/work/W2410288554> ?p ?o ?g. }
- W2410288554 endingPage "1165" @default.
- W2410288554 startingPage "1157" @default.
- W2410288554 abstract "A series of multitarget directed propargylamines, as well as other differently susbstituted piperidines have been screened as potential modulators of neuronal nicotinic acetylcholine receptors (nAChRs). Most of them showed antagonist actions on α7 nAChRs. Especially, compounds 13, 26, and 38 displayed submicromolar IC50 values on homomeric α7 nAChRs, whereas they were less effective on heteromeric α3β4 and α4β2 nAChRs (up to 20-fold higher IC50 values in the case of 13). Antagonism was concentration dependent and noncompetitive, suggesting that these compounds behave as negative allosteric modulators of nAChRs. Upon the study of a series of less complex derivatives, the N-benzylpiperidine motif, common to these compounds, was found to be the main pharmacophoric group. Thus, 2-(1-benzylpiperidin-4-yl)-ethylamine (48) showed an inhibitory potency comparable to the one of the previous compounds and also a clear preference for α7 nAChRs. In a neuroblastoma cell line, representative compounds 13 and 48 also inhibited, in a concentration-dependent manner, cytosolic Ca2+ signals mediated by nAChRs. Finally, compounds 38 and 13 inhibited 5-HT3A serotonin receptors whereas they had no effect on α1 glycine receptors. Given the multifactorial nature of many pathologies in which nAChRs are involved, these piperidine antagonists could have a therapeutic potential in cases where cholinergic activity has to be negatively modulated." @default.
- W2410288554 created "2016-06-24" @default.
- W2410288554 creator A5011610277 @default.
- W2410288554 creator A5017665436 @default.
- W2410288554 creator A5018104052 @default.
- W2410288554 creator A5020190176 @default.
- W2410288554 creator A5044493452 @default.
- W2410288554 creator A5054480308 @default.
- W2410288554 creator A5054844397 @default.
- W2410288554 creator A5071876543 @default.
- W2410288554 creator A5082905681 @default.
- W2410288554 creator A5084716960 @default.
- W2410288554 date "2016-06-10" @default.
- W2410288554 modified "2023-10-16" @default.
- W2410288554 title "<i>N</i>-Benzylpiperidine Derivatives as α7 Nicotinic Receptor Antagonists" @default.
- W2410288554 cites W1548483078 @default.
- W2410288554 cites W1573139078 @default.
- W2410288554 cites W1981581272 @default.
- W2410288554 cites W1982706802 @default.
- W2410288554 cites W1992326577 @default.
- W2410288554 cites W2001220427 @default.
- W2410288554 cites W2010022125 @default.
- W2410288554 cites W2015160568 @default.
- W2410288554 cites W2021909520 @default.
- W2410288554 cites W2025223727 @default.
- W2410288554 cites W2027131229 @default.
- W2410288554 cites W2033154101 @default.
- W2410288554 cites W2041909191 @default.
- W2410288554 cites W2043158072 @default.
- W2410288554 cites W2044354004 @default.
- W2410288554 cites W2046087123 @default.
- W2410288554 cites W2055686915 @default.
- W2410288554 cites W2057320515 @default.
- W2410288554 cites W2058945187 @default.
- W2410288554 cites W2060241841 @default.
- W2410288554 cites W2061287334 @default.
- W2410288554 cites W2064864270 @default.
- W2410288554 cites W2070115473 @default.
- W2410288554 cites W2070151592 @default.
- W2410288554 cites W2078277622 @default.
- W2410288554 cites W2086808366 @default.
- W2410288554 cites W2088442234 @default.
- W2410288554 cites W2089013306 @default.
- W2410288554 cites W2091478089 @default.
- W2410288554 cites W2121003575 @default.
- W2410288554 cites W2122512713 @default.
- W2410288554 cites W2127401626 @default.
- W2410288554 cites W2131697773 @default.
- W2410288554 cites W2138645881 @default.
- W2410288554 cites W2145810295 @default.
- W2410288554 cites W2155997108 @default.
- W2410288554 cites W2156076504 @default.
- W2410288554 cites W2166955092 @default.
- W2410288554 cites W2405720805 @default.
- W2410288554 cites W570865489 @default.
- W2410288554 cites W962937402 @default.
- W2410288554 cites W2012464665 @default.
- W2410288554 doi "https://doi.org/10.1021/acschemneuro.6b00122" @default.
- W2410288554 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27254782" @default.
- W2410288554 hasPublicationYear "2016" @default.
- W2410288554 type Work @default.
- W2410288554 sameAs 2410288554 @default.
- W2410288554 citedByCount "7" @default.
- W2410288554 countsByYear W24102885542017 @default.
- W2410288554 countsByYear W24102885542020 @default.
- W2410288554 countsByYear W24102885542021 @default.
- W2410288554 countsByYear W24102885542023 @default.
- W2410288554 crossrefType "journal-article" @default.
- W2410288554 hasAuthorship W2410288554A5011610277 @default.
- W2410288554 hasAuthorship W2410288554A5017665436 @default.
- W2410288554 hasAuthorship W2410288554A5018104052 @default.
- W2410288554 hasAuthorship W2410288554A5020190176 @default.
- W2410288554 hasAuthorship W2410288554A5044493452 @default.
- W2410288554 hasAuthorship W2410288554A5054480308 @default.
- W2410288554 hasAuthorship W2410288554A5054844397 @default.
- W2410288554 hasAuthorship W2410288554A5071876543 @default.
- W2410288554 hasAuthorship W2410288554A5082905681 @default.
- W2410288554 hasAuthorship W2410288554A5084716960 @default.
- W2410288554 hasBestOaLocation W24102885542 @default.
- W2410288554 hasConcept C104292427 @default.
- W2410288554 hasConcept C104317684 @default.
- W2410288554 hasConcept C134018914 @default.
- W2410288554 hasConcept C166342909 @default.
- W2410288554 hasConcept C170493617 @default.
- W2410288554 hasConcept C185592680 @default.
- W2410288554 hasConcept C188987157 @default.
- W2410288554 hasConcept C22885893 @default.
- W2410288554 hasConcept C2776038425 @default.
- W2410288554 hasConcept C2776104367 @default.
- W2410288554 hasConcept C2776885963 @default.
- W2410288554 hasConcept C2781462491 @default.
- W2410288554 hasConcept C2909754679 @default.
- W2410288554 hasConcept C55493867 @default.
- W2410288554 hasConcept C71240020 @default.
- W2410288554 hasConcept C80161118 @default.
- W2410288554 hasConcept C86803240 @default.
- W2410288554 hasConcept C98274493 @default.
- W2410288554 hasConceptScore W2410288554C104292427 @default.