| AID611805 | Inhibition of RAMH-induced dipsogenia in Long Evans rat administered as po 15 mins prior to RAMH challenge | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID648457 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity. |
| AID611542 | Inhibition of norepinephrine transporter | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611540 | Inhibition of adrenergic alpha 1A receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611527 | Antagonist activity at histamine H3 receptor in rat cortical membrane | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID630097 | Displacement of [3H]NAMH from human H3R expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity. |
| AID611539 | Inhibition of muscarinic M2 receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611531 | Antagonist activity against rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611633 | Aqueous solubility of the compound at pH 2 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611535 | Selectivity for human histamine H3 receptor over human H4 receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611631 | Inhibition of recombinant human dopamine transporter | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611528 | Dissociation constant, pKa of the compound | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611536 | Inhibition of human histamine H1 receptor at 10 uM | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611806 | Toxicity in rat central nervous system assessed as changes in behavioral response at 10 to 300 mg/kg, po measured from 15 mins through 6 hrs by Irwin test | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611529 | Antagonist activity against human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611803 | Toxicity in monkey assessed as changes in respiratory function after 28 days | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID648452 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv and 5 mg/kg, po | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity. |
| AID1071994 | Displacement of [3H]NAMH from rat histamine H3 receptor transfected in CHO cells | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity. |
| AID611802 | Toxicity in monkey assessed as changes in cardiovascular function after 28 days | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611727 | Mutagenic activity in human peripheral blood lymphocytes by micronucleus test in absence metabolic activation | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611634 | Aqueous solubility of the compound at pH 7.4 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611804 | Inhibition of RAMH-induced dipsogenia in ip dosed Long Evans rat administered 15 mins prior to RAMH challenge | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611728 | Mutagenic activity in Salmonella Typhimurium by Ames test | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID1201926 | Binding affinity to human histamine H3 receptor | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity. |
| AID611800 | Toxicity in rat up to 28 days | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611808 | Drug level in rat brain at 100 mg/kg, po administered after 1 hr post dosing | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611532 | Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611807 | Toxicity in rat central nervous system assessed as side effects up to 100 mg/kg, po measured from 15 mins through 6 hrs by Irwin test | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID648458 | Ratio of drug level in brain to plasma in Sprague-Dawley rat at 10 mg/kg, ip after 1 hr | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity. |
| AID611537 | Inhibition of human histamine H2 receptor at 10 uM | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611534 | Selectivity for human histamine H3 receptor over human H2 receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611517 | Displacement of [3H]NAMH from human histamine H3 receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611543 | Inhibition of PDE3 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID1071995 | Displacement of [3H]NAMH from human histamine H3 receptor transfected in CHO cells | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity. |
| AID611809 | Therapeutic index in rat dispogenia model | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611729 | Mutagenic activity in Salmonella Typhimurium by Ames test in presence of rat liver S9 fraction | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID1201927 | Binding affinity to rat histamine H3 receptor | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity. |
| AID618581 | Displacement of [3H]NAMH from human cloned histamine 3 receptor expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity. |
| AID630098 | Displacement of [3H]NAMH from rat H3R expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity. |
| AID648455 | Displacement of [3H]NAMH from human cloned 5HT3 receptor expressed in CHO cells | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity. |
| AID611630 | Inhibition of human PARP1 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID622483 | Displacement of [3H]-NAMH from human histamine H3 receptor expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists. |
| AID611538 | Inhibition of human histamine H4 receptor at 10 uM | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611801 | Toxicity in monkey up to 28 days | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611519 | Distribution coefficient log D of the compound at pH 7.4 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611632 | Inhibition of recombinant human norepinephrine transporter | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611635 | Apparent permeability across human Caco2 cell membrane | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611541 | Inhibition of dopamine transporter | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611533 | Selectivity for human histamine H3 receptor over human H1 receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID648453 | Half life in Sprague-Dawley rat at 1 mg/kg, iv and 5 mg/kg, po | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity. |
| AID648454 | Displacement of [3H]NAMH from rat cloned 5HT3 receptor expressed in CHO cells | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H₃ receptor antagonists with potent cognition enhancing activity. |
| AID622486 | Displacement of [3H]-NAMH from rat histamine H3 receptor expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists. |
| AID611636 | Permeability across human Caco2 cells expressing P-gp assessed as directional transport | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID618582 | Displacement of [3H]NAMH from rat cloned histamine 3 receptor expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity. |
| AID611530 | Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611518 | Displacement of [3H]NAMH from rat histamine H3 receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611725 | Inhibition of recombinant human ERG channel expressed in human HEK 293 cells by patch clamp assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| AID611726 | Mutagenic activity in human peripheral blood lymphocytes by micronucleus test in presence metabolic activation | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |