PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 20813479-0 2011 NMR spectroscopy and surface tension measurements applied to the study of self-association of casopitant mesylate, a novel NK1 antagonist. casopitant 94-104 tachykinin receptor 1 Homo sapiens 123-126 22020354-2 2011 Casopitant, a selective NK1 antagonist that achieves nearly complete receptor occupancy was studied in 2 randomized, placebo-controlled, double-blind, Phase II trials in depressed outpatients to test the hypothesis that nearly complete NK1 receptor occupancy is required to achieve antidepressant efficacy. casopitant 0-10 tachykinin receptor 1 Homo sapiens 24-27 22020354-2 2011 Casopitant, a selective NK1 antagonist that achieves nearly complete receptor occupancy was studied in 2 randomized, placebo-controlled, double-blind, Phase II trials in depressed outpatients to test the hypothesis that nearly complete NK1 receptor occupancy is required to achieve antidepressant efficacy. casopitant 0-10 tachykinin receptor 1 Homo sapiens 236-248 21993526-11 2012 CONCLUSION: These results indicate that after chronic dosing, casopitant can achieve a degree of NK(1) receptor occupancy higher than those that have previously been tested in studies of clinical depression. casopitant 62-72 tachykinin receptor 1 Homo sapiens 97-111 21149541-3 2011 Casopitant is shown to be a substrate, an inhibitor, and an inducer of CYP3A4, and, because of this complex behavior, it was difficult to identify the primary mechanism by which it may give rise to drug-drug interactions (DDIs) of clinical relevance. casopitant 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 20813479-1 2011 The aggregation behaviour of casopitant mesylate, a new NK1 antagonist drug, was investigated by means of NMR spectroscopy and surface tension measurements. casopitant 29-48 tachykinin receptor 1 Homo sapiens 56-59 20124517-1 2010 Casopitant, an antiemetic, is a neurokinin-1 receptor antagonist metabolized primarily by cytochrome P450 3A4 (CYP3A4). casopitant 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-109 20124517-1 2010 Casopitant, an antiemetic, is a neurokinin-1 receptor antagonist metabolized primarily by cytochrome P450 3A4 (CYP3A4). casopitant 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 111-117 20124517-8 2010 Coadministration of casopitant with strong inhibitors of CYP3A is likely to increase plasma exposure of casopitant, whereas coadministration with strong inducers of CYP3A is likely to decrease casopitant exposure and compromise efficacy. casopitant 20-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-62 19428297-0 2009 Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenic chemotherapy: a randomised, double-blind, placebo-controlled trial. casopitant 23-42 tachykinin receptor 1 Homo sapiens 46-73 18600583-1 2008 Casopitant, an inhibitor of the neurokinin-1 receptor, and its mesylate salt, are being developed by GlaxoSmithKline plc for the potential treatment of chemotherapy-induced nausea and vomiting (CINV), post-operative nausea and vomiting (PONV), as well as for anxiety, depression and insomnia. casopitant 0-10 heparan sulfate proteoglycan 2 Homo sapiens 117-120