FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2116573364> ?p ?o ?g. }

• W2116573364 endingPage "734" @default.
• W2116573364 startingPage "725" @default.
• W2116573364 abstract "The in vitro pharmacological properties of a novel cholinergic channel ligand, A-85380 [3-(2(S)-azetidinylmethoxy)pyridine], were examined using tissue preparations that express different putative nAChR subtypes. In radioligand binding studies, A-85380 is shown to be a potent and selective ligand for the human alpha 4 beta 2 nAChR subtype (Ki = 0.05 + 0.01 nM) relative to the human alpha 7 (Ki = 148 +/- 13 nM) and the muscle alpha 1 beta 1 dg subtype expressed in Torpedo electroplax (Ki = 314 +/- 12 nM). The R-enantiomer of A-85380, A-159470, displays little enantioselectivity towards the alpha 4 beta 2 and alpha 1 beta 1 delta gamma subtypes but does not display 12-fold enantioselectivity towards the alpha 7 subtype (Ki = 1275 +/- 199 nM). (+)- and(-)-Epibatidine display similar potencies at the human human alpha 4 beta 2 (Ki = 0.04 +/- 0.02 nM and 0.07 +/- 0.02 nM, respectively), human alpha 7 (Ki = 16 +/- 2 nM and 22 +/- 3 nM, respectively) and muscle alpha 1 beta 1 delta gamma g (Ki = 2.5 +/- 0.9 nM and 5.7 +/- 1.0 nM, respectively) nAChRs. Functionally, A-85380 is a potent activator of cation efflux through the human alpha 4 beta 2 (EC50 = 0.7 +/- 0.1 microM) and ganglionic (EC50 = 0.8 +/- 0.09 microM) subtypes, effects that are attenuated by pretreatment with mecamylamine (10 microM). Further, A-85380 can activate (EC50 = 8.9 +/- 1.9 microM) currents through channels formed by injection of the human alpha 7 subunit into Xenopus oocytes, effects that are attenuated by pretreatment with the alpha 7 nAChR antagonist, methyllycaconitine (10 nM). In all cases, A-85380 is more potent than (-)-nicotine but less potent than (+/-)-epibatidine. In neurotransmitter release studies, A-85380 stimulates the release of dopamine with an EC 50 value of 0.003 +/- 0.001 microM which is equipotent to (+/-)-epibatidine, and 20-fold more potent than (-)-nicotine (EC50 = 0.04 +/- 0.009 microM). Thus, A-85380 displays a profile of robust activation of a number of nAChR subtypes with substantially less affinity for [125I] alpha-BgT sites than [3H](-)-cytisine sites, suggesting that it may serve as a more selective pharmacologic probe for the alpha 4 beta 2 subtype relative to the alpha 7 and alpha 1 beta 1 delta g nAChRs than (+/-)-epibatidine." @default.
• W2116573364 created "2016-06-24" @default.
• W2116573364 creator A5001947667 @default.
• W2116573364 creator A5002585607 @default.
• W2116573364 creator A5008071761 @default.
• W2116573364 creator A5009413082 @default.
• W2116573364 creator A5013364999 @default.
• W2116573364 creator A5029000472 @default.
• W2116573364 creator A5038977774 @default.
• W2116573364 creator A5044940190 @default.
• W2116573364 creator A5045300839 @default.
• W2116573364 creator A5046761678 @default.
• W2116573364 creator A5055726650 @default.
• W2116573364 creator A5056916898 @default.
• W2116573364 creator A5071528832 @default.
• W2116573364 creator A5073992167 @default.
• W2116573364 creator A5078928735 @default.
• W2116573364 date "1996-06-01" @default.
• W2116573364 modified "2023-09-23" @default.
• W2116573364 title "A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: In Vitro pharmacological properties of a novel, high affinity α4β2 nicotinic acetylcholine receptor ligand" @default.
• W2116573364 cites W1579522803 @default.
• W2116573364 cites W1900806927 @default.
• W2116573364 cites W1974100135 @default.
• W2116573364 cites W1989901068 @default.
• W2116573364 cites W1991630622 @default.
• W2116573364 cites W1994322758 @default.
• W2116573364 cites W2005274709 @default.
• W2116573364 cites W2007226311 @default.
• W2116573364 cites W2038995429 @default.
• W2116573364 cites W2041281912 @default.
• W2116573364 cites W2044727164 @default.
• W2116573364 cites W2045122897 @default.
• W2116573364 cites W2048489717 @default.
• W2116573364 cites W2049949416 @default.
• W2116573364 cites W2053656727 @default.
• W2116573364 cites W2061569848 @default.
• W2116573364 cites W2061675635 @default.
• W2116573364 cites W2066628109 @default.
• W2116573364 cites W2070295245 @default.
• W2116573364 cites W2074631079 @default.
• W2116573364 cites W2111148750 @default.
• W2116573364 cites W2174802300 @default.
• W2116573364 cites W2953274112 @default.
• W2116573364 doi "https://doi.org/10.1016/0028-3908(96)84644-2" @default.
• W2116573364 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8887981" @default.
• W2116573364 hasPublicationYear "1996" @default.
• W2116573364 type Work @default.
• W2116573364 sameAs 2116573364 @default.
• W2116573364 citedByCount "129" @default.
• W2116573364 countsByYear W21165733642012 @default.
• W2116573364 countsByYear W21165733642013 @default.
• W2116573364 countsByYear W21165733642014 @default.
• W2116573364 countsByYear W21165733642015 @default.
• W2116573364 countsByYear W21165733642016 @default.
• W2116573364 countsByYear W21165733642017 @default.
• W2116573364 countsByYear W21165733642018 @default.
• W2116573364 countsByYear W21165733642019 @default.
• W2116573364 countsByYear W21165733642020 @default.
• W2116573364 countsByYear W21165733642021 @default.
• W2116573364 crossrefType "journal-article" @default.
• W2116573364 hasAuthorship W2116573364A5001947667 @default.
• W2116573364 hasAuthorship W2116573364A5002585607 @default.
• W2116573364 hasAuthorship W2116573364A5008071761 @default.
• W2116573364 hasAuthorship W2116573364A5009413082 @default.
• W2116573364 hasAuthorship W2116573364A5013364999 @default.
• W2116573364 hasAuthorship W2116573364A5029000472 @default.
• W2116573364 hasAuthorship W2116573364A5038977774 @default.
• W2116573364 hasAuthorship W2116573364A5044940190 @default.
• W2116573364 hasAuthorship W2116573364A5045300839 @default.
• W2116573364 hasAuthorship W2116573364A5046761678 @default.
• W2116573364 hasAuthorship W2116573364A5055726650 @default.
• W2116573364 hasAuthorship W2116573364A5056916898 @default.
• W2116573364 hasAuthorship W2116573364A5071528832 @default.
• W2116573364 hasAuthorship W2116573364A5073992167 @default.
• W2116573364 hasAuthorship W2116573364A5078928735 @default.
• W2116573364 hasConcept C116569031 @default.
• W2116573364 hasConcept C159110408 @default.
• W2116573364 hasConcept C170493617 @default.
• W2116573364 hasConcept C185592680 @default.
• W2116573364 hasConcept C188987157 @default.
• W2116573364 hasConcept C199360897 @default.
• W2116573364 hasConcept C202751555 @default.
• W2116573364 hasConcept C2775944032 @default.
• W2116573364 hasConcept C2776174256 @default.
• W2116573364 hasConcept C2779570518 @default.
• W2116573364 hasConcept C2780928369 @default.
• W2116573364 hasConcept C41008148 @default.
• W2116573364 hasConcept C49453240 @default.
• W2116573364 hasConcept C55493867 @default.
• W2116573364 hasConcept C64943373 @default.
• W2116573364 hasConcept C67847695 @default.
• W2116573364 hasConcept C71240020 @default.
• W2116573364 hasConcept C71924100 @default.
• W2116573364 hasConcept C80161118 @default.
• W2116573364 hasConceptScore W2116573364C116569031 @default.
• W2116573364 hasConceptScore W2116573364C159110408 @default.
• W2116573364 hasConceptScore W2116573364C170493617 @default.
• W2116573364 hasConceptScore W2116573364C185592680 @default.

• next