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Binding to Nicotinic Receptor Subtypes from US Patent US11667638: "4-substitued cytisine analogues"
Assay data:50 Active, 3 Activity ≤ 1 nM, 50 Activity ≤ 1 µM, 50 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of human alpha4beta4 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human alpha4beta2 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method
Inhibition of human recombinant nAChRalpha4/beta2 incubated for 120 mins by radiometric scintillation counting method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human alpha4beta2 nAChR at 10 uM relative to control by Ion flux assay
Antagonist activity at human alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential in presence of BAPTA-AM at 100 nM by two-electrode voltage clamp method
Antagonist activity at human alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential in presence of BAPTA-AM at 10 uM by two-electrode voltage clamp method
Antagonist activity at human alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential at 10 uM by two-electrode voltage clamp method
Antagonist activity at human alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential at 1 uM by two-electrode voltage clamp method
Partial agonist activity at low sensitivity isoform human (alpha4)3(beta2)2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response at holding potential of -50 mV by two-electrode voltage clamp technique relative to control
Assay data:4 Tested
Partial agonist activity at high sensitivity isoform human (alpha4)2(beta2)3 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response at holding potential of -50 mV by two-electrode voltage clamp technique relative to control
Assay data:3 Tested
Partial agonist activity at low sensitivity isoform human (alpha4)3(beta2)2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response at holding potential of -50 mV by two-electrode voltage clamp technique
Assay data:2 Active, 4 Tested
Partial agonist activity at high sensitivity isoform human (alpha4)2(beta2)3 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response at holding potential of -50 mV by two-electrode voltage clamp technique
Assay data:3 Active, 2 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [3H]epibatidine from human alpha4beta2 nAChR expressed in HEK293 cell membrane incubated for 3 hrs by scinitillation counting analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 6 Tested
Displacement of [3H]-epibatidine from human alpha4beta2 nAChR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by overnight incubation with [3H]-epibatidine by gamma liquid scintilation counting analysis
Assay data:16 Active, 16 Activity ≤ 1 µM, 16 Tested
Effect on human nAChR alpha4beta2 expressed in Xenopus laevis oocytes at 10 uM at holding potential of -70 mV incubated for 5 mins by voltage-clamp based electrophysiological method
Inhibition of nAChR alpha4beta2 receptor (unknown origin) at 10 uM relative to control
N_NEURO_A4B2 Eurofins SafetyScreen44 (BI)
SummaryRelated BioAssays by Target
nAChR(a4/b2) Eurofins SafetyScreen (Other)
Non-competitive antagonist activity at human (alpha4)3(beta2)2 nAChR expressed in Xenopus laevis oocytes decrease in acetylcholine-induced maximum current with non-significant change in Ach potency at IC50 pretreated for 30 secs followed by co-application with acetylcholine measured at holding potential of -60 mV by two-electrode voltage-clamp method
Assay data:4 Active, 4 Tested
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