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Neuroprotective activity against MPTP-induced neurotoxicity in BALB/c albino mouse model assessed as alleviation of MPTP-induced nigrostriatal dopaminergic neuronal damage by measuring increase in number of TH-postivie neurons in substantia nigra at 10 mg/kg, ip preadministered with compound for 1 hrs followed by MPTP addition and measured 11 days after first MPTP addition by immunohistological staining analysis (Rvb = 66 +/- 1.41%)
Assay data:2 Tested
SummaryPubMed Citation
Neuroprotective activity against MPTP-induced Parkinson's disease BALB/c albino mouse model assessed as restoration of motor function by measuring increase in hanging time value at 10 mg/kg, ip preadministered with compound for 1 hrs followed by MPTP addition and measured 10 days after first MPTP addition by hanging test relative to control
Toxicity in MPTP-induced parkinsons's disease BALB/c albino mouse model assessed as body weight loss at 10 mg/kg, ip preadministered with compound for 1 hrs followed by MPTP-addition and measured 10 days after first MPTP addition
Toxicity in MPTP-induced parkinsons's disease BALB/c albino mouse model assessed as body weight loss at 10 mg/kg, ip preadministered with compound for 1 hrs followed by MPTP-addition and measured 5 days after first MPTP addition
Neuroprotective activity against MPTP-induced Parkinson's disease BALB/c albino mouse model assessed as restoration of step-through latency values at 10 mg/kg, ip preadministered with compound for 1 hrs followed by MPTP addition and measured 10 days after first MPTP addition by step-through passive avoidance test
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed Citation
Permeability coefficient of compound in PBS buffer at pH 7.4 at 100 uM incubated for 4 hrs by PAMPA-BBB assay
Assay data:3 Tested
Permeability of compound in PBS buffer at pH 7.4 at 100 uM incubated for 4 hrs by PAMPA-BBB assay
Stability of compound in PBS buffer assessed as parent compound remaining at pH 7.4 measured after 30 days by RP-HPLC/UV/Vis spectroscopic analysis
Stability of compound in PBS buffer assessed as parent compound remaining at pH 2.0 measured after 30 days by RP-HPLC/UV/Vis spectroscopic analysis
Stability of compound in PBS buffer assessed as parent compound remaining at pH 7.4 incubated for 24 hrs by UV/Vis spectroscopic analysis
Stability of compound in PBS buffer assessed as parent compound remaining at pH 2.0 incubated for 24 hrs by UV/Vis spectroscopic analysis
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 24 hrs by MTT assay
Assay data:5 Tested
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 24 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability at 100 uM incubated for 24 hrs by MTT assay relative to control
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 100 uM incubated for 24 hrs by MTT assay relative to control
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 100 uM incubated for 24 hrs by MTT assay relative to control
Agonist activity at human NTSR1 expressed in HEK293 cells assessed as Galphaq-mediated modulation of IP production incubated for 90 mins by IP-one HTRF assay
Assay data:7 Active, 5 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Selectivity index, ratio of Kd for human NTSR1 transfected in HEK293 cells in the presence of [Leu3H]NT(8-13) to Kd for human NTSR2 transfected in HEK293 cells in the presence of [Leu3H]NT(8-13)
Assay data:1 Tested
Binding affinity to human NTSR2 transfected in HEK293 cells assessed as inhibition constant incubated for 60 mins in the presence of [Leu3H]NT(8-13) by radioligand competition binding assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 7 Tested
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