PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 31786978-5 2020 This has led to development of RB150, an orally active prodrug of the specific and selective APA inhibitor, EC33. firibastat 31-36 glutamyl aminopeptidase Rattus norvegicus 93-96 31786978-6 2020 Orally administered RB150 crosses the gastrointestinal and blood-brain barriers, enters the brain where it generates 2 active molecules of EC33 that block brain APA activity. firibastat 20-25 glutamyl aminopeptidase Rattus norvegicus 161-164 15136730-5 2004 We developed RB150, a prodrug of the specific and selective APA inhibitor, EC33. firibastat 13-18 glutamyl aminopeptidase Rattus norvegicus 60-63 31067198-3 2019 We have also shown that injection of the specific and selective aminopeptidase A inhibitor, (3S)-3-amino-4-sulfanyl-butane-1-sulfonic acid (EC33), by central route or its prodrug, RB150/firibastat, by oral route inhibited brain aminopeptidase A activity and blocked the formation of brain angiotensin III, normalizing blood pressure in hypertensive rats. firibastat 180-185 glutamyl aminopeptidase Rattus norvegicus 64-80 31067198-3 2019 We have also shown that injection of the specific and selective aminopeptidase A inhibitor, (3S)-3-amino-4-sulfanyl-butane-1-sulfonic acid (EC33), by central route or its prodrug, RB150/firibastat, by oral route inhibited brain aminopeptidase A activity and blocked the formation of brain angiotensin III, normalizing blood pressure in hypertensive rats. firibastat 186-196 glutamyl aminopeptidase Rattus norvegicus 64-80 31115779-4 2019 This identified brain APA as a potential therapeutic target for the treatment of hypertension, leading to the development of RB150/firibastat, an orally active prodrug of the specific and selective APA inhibitor, EC33. firibastat 125-131 glutamyl aminopeptidase Rattus norvegicus 22-25 31115779-4 2019 This identified brain APA as a potential therapeutic target for the treatment of hypertension, leading to the development of RB150/firibastat, an orally active prodrug of the specific and selective APA inhibitor, EC33. firibastat 125-131 glutamyl aminopeptidase Rattus norvegicus 198-201 31115779-4 2019 This identified brain APA as a potential therapeutic target for the treatment of hypertension, leading to the development of RB150/firibastat, an orally active prodrug of the specific and selective APA inhibitor, EC33. firibastat 131-141 glutamyl aminopeptidase Rattus norvegicus 22-25 31115779-4 2019 This identified brain APA as a potential therapeutic target for the treatment of hypertension, leading to the development of RB150/firibastat, an orally active prodrug of the specific and selective APA inhibitor, EC33. firibastat 131-141 glutamyl aminopeptidase Rattus norvegicus 198-201 31115779-5 2019 When given orally, RB150/firibastat crosses the gastrointestinal and blood-brain barriers, enters the brain, and generates two active molecules of EC33 which inhibit brain APA activity, blocking brain angiotensin III formation, and decrease blood pressure for several hours in hypertensive rats. firibastat 19-24 glutamyl aminopeptidase Rattus norvegicus 172-175 31115779-5 2019 When given orally, RB150/firibastat crosses the gastrointestinal and blood-brain barriers, enters the brain, and generates two active molecules of EC33 which inhibit brain APA activity, blocking brain angiotensin III formation, and decrease blood pressure for several hours in hypertensive rats. firibastat 25-35 glutamyl aminopeptidase Rattus norvegicus 172-175 30531435-1 2019 AIMS: Inhibition of brain angiotensin III by central infusion of aminopeptidase A (APA) inhibitor firibastat (RB150) inhibits sympathetic hyperactivity and heart failure in rats after myocardial infarction (MI). firibastat 98-108 glutamyl aminopeptidase Rattus norvegicus 65-81 30531435-1 2019 AIMS: Inhibition of brain angiotensin III by central infusion of aminopeptidase A (APA) inhibitor firibastat (RB150) inhibits sympathetic hyperactivity and heart failure in rats after myocardial infarction (MI). firibastat 98-108 glutamyl aminopeptidase Rattus norvegicus 83-86 30531435-1 2019 AIMS: Inhibition of brain angiotensin III by central infusion of aminopeptidase A (APA) inhibitor firibastat (RB150) inhibits sympathetic hyperactivity and heart failure in rats after myocardial infarction (MI). firibastat 110-115 glutamyl aminopeptidase Rattus norvegicus 65-81 30531435-1 2019 AIMS: Inhibition of brain angiotensin III by central infusion of aminopeptidase A (APA) inhibitor firibastat (RB150) inhibits sympathetic hyperactivity and heart failure in rats after myocardial infarction (MI). firibastat 110-115 glutamyl aminopeptidase Rattus norvegicus 83-86 30531435-7 2019 Both s.c. and oral firibastat inhibited brain APA and attenuated left ventricle dysfunction. firibastat 19-29 glutamyl aminopeptidase Rattus norvegicus 46-49 28968260-0 2018 Central antihypertensive effects of chronic treatment with RB150: an orally active aminopeptidase A inhibitor in deoxycorticosterone acetate-salt rats. firibastat 59-64 glutamyl aminopeptidase Rattus norvegicus 83-99 28968260-4 2018 We developed RB150, a prodrug of the specific and selective APA inhibitor, EC33. firibastat 13-18 glutamyl aminopeptidase Rattus norvegicus 60-63 24697296-7 2014 This identified brain APA as a potential therapeutic target for the treatment of hypertension, which has led to the development of potent orally active APA inhibitors, such as RB150. firibastat 176-181 glutamyl aminopeptidase Rattus norvegicus 22-25 24697296-7 2014 This identified brain APA as a potential therapeutic target for the treatment of hypertension, which has led to the development of potent orally active APA inhibitors, such as RB150. firibastat 176-181 glutamyl aminopeptidase Rattus norvegicus 152-155 24697296-8 2014 RB150 administered orally in hypertensive DOCA (deoxycorticosteroneacetate)-salt rats or SHRs (spontaneously hypertensive rats) crosses the intestinal, hepatic and blood-brain barriers, enters the brain, generates two active molecules of EC33 which inhibit brain APA activity, block the formation of brain AngIII and normalize BP for several hours. firibastat 0-5 glutamyl aminopeptidase Rattus norvegicus 263-266 22710644-5 2012 We demonstrated here the antihypertensive effects of RB150, a prodrug of the specific and selective aminopeptidase A inhibitor, EC33, in spontaneously hypertensive rats, a model of human essential hypertension. firibastat 53-58 glutamyl aminopeptidase Rattus norvegicus 100-116 22710644-6 2012 Oral administration of RB150 in conscious spontaneously hypertensive rats inhibited brain aminopeptidase A activity, demonstrating the central bioavailability of RB150 and its ability to generate EC33 into the brain. firibastat 23-28 glutamyl aminopeptidase Rattus norvegicus 90-106 22710644-6 2012 Oral administration of RB150 in conscious spontaneously hypertensive rats inhibited brain aminopeptidase A activity, demonstrating the central bioavailability of RB150 and its ability to generate EC33 into the brain. firibastat 162-167 glutamyl aminopeptidase Rattus norvegicus 90-106 18194430-5 2008 This justifies the development of potent systemically active APA inhibitors, such as RB150, as prototypes of a new class of antihypertensive agents for the treatment of certain forms of hypertension. firibastat 85-90 glutamyl aminopeptidase Rattus norvegicus 61-64 15136730-9 2004 in conscious DOCA-salt rats inhibited brain APA activity and markedly reduced blood pressure for up to 24 h. These results demonstrate the crucial role of brain APA as a candidate target for the treatment of hypertension and suggest that RB150, a potent systemically active APA inhibitor, could be the prototype of a new class of antihypertensive agents for the treatment of certain forms of hypertension. firibastat 238-243 glutamyl aminopeptidase Rattus norvegicus 44-47 15136730-9 2004 in conscious DOCA-salt rats inhibited brain APA activity and markedly reduced blood pressure for up to 24 h. These results demonstrate the crucial role of brain APA as a candidate target for the treatment of hypertension and suggest that RB150, a potent systemically active APA inhibitor, could be the prototype of a new class of antihypertensive agents for the treatment of certain forms of hypertension. firibastat 238-243 glutamyl aminopeptidase Rattus norvegicus 161-164 15136730-9 2004 in conscious DOCA-salt rats inhibited brain APA activity and markedly reduced blood pressure for up to 24 h. These results demonstrate the crucial role of brain APA as a candidate target for the treatment of hypertension and suggest that RB150, a potent systemically active APA inhibitor, could be the prototype of a new class of antihypertensive agents for the treatment of certain forms of hypertension. firibastat 238-243 glutamyl aminopeptidase Rattus norvegicus 161-164 33683322-0 2021 Brain ACE2 Activation Following Brain Aminopeptidase A Blockade by Firibastat in Salt-dependent Hypertension. firibastat 67-77 glutamyl aminopeptidase Rattus norvegicus 38-54 33683322-3 2021 Blocking brain angiotensin III formation by the APA inhibitor prodrug RB150/firibastat normalizes arterial blood pressure in hypertensive DOCA-salt rats without inducing angiotensin II accumulation. firibastat 70-75 glutamyl aminopeptidase Rattus norvegicus 48-51 33683322-3 2021 Blocking brain angiotensin III formation by the APA inhibitor prodrug RB150/firibastat normalizes arterial blood pressure in hypertensive DOCA-salt rats without inducing angiotensin II accumulation. firibastat 76-86 glutamyl aminopeptidase Rattus norvegicus 48-51 33683322-5 2021 We found that the intracerebroventricular administration of RB150/firibastat in conscious DOCA-salt rats both inhibited brain APA activity and induced an increase in brain ACE2 activity. firibastat 60-65 glutamyl aminopeptidase Rattus norvegicus 126-129 33683322-5 2021 We found that the intracerebroventricular administration of RB150/firibastat in conscious DOCA-salt rats both inhibited brain APA activity and induced an increase in brain ACE2 activity. firibastat 66-76 glutamyl aminopeptidase Rattus norvegicus 126-129 34020248-2 2021 Oral administration of firibastat, an APA inhibitor prodrug, in hypertensive rats, inhibits brain APA activity, blocks brain angiotensin III formation and decreases BP. firibastat 23-33 glutamyl aminopeptidase Rattus norvegicus 38-41 34020248-2 2021 Oral administration of firibastat, an APA inhibitor prodrug, in hypertensive rats, inhibits brain APA activity, blocks brain angiotensin III formation and decreases BP. firibastat 23-33 glutamyl aminopeptidase Rattus norvegicus 98-101 33683322-6 2021 Then, we showed that the decreases in blood pressure and arginine-vasopressin release resulting from brain APA inhibition with RB150/firibastat were reduced if ACE2 was concomitantly inhibited by MLN4760, a potent ACE2 inhibitor, or if the Mas receptor (MasR) was blocked by A779, a MasR antagonist. firibastat 127-132 glutamyl aminopeptidase Rattus norvegicus 107-110 33683322-6 2021 Then, we showed that the decreases in blood pressure and arginine-vasopressin release resulting from brain APA inhibition with RB150/firibastat were reduced if ACE2 was concomitantly inhibited by MLN4760, a potent ACE2 inhibitor, or if the Mas receptor (MasR) was blocked by A779, a MasR antagonist. firibastat 133-143 glutamyl aminopeptidase Rattus norvegicus 107-110 33683322-7 2021 Our findings suggest that in the brain, the increase in ACE2 activity resulting from APA inhibition by RB150/firibastat treatment, subsequently increasing angiotensin 1-7 and activating the MasR while blocking angiotensin III formation, contributes to the antihypertensive effect and the decrease in arginine-vasopressin release induced by RB150/firibastat. firibastat 103-108 glutamyl aminopeptidase Rattus norvegicus 85-88 33683322-7 2021 Our findings suggest that in the brain, the increase in ACE2 activity resulting from APA inhibition by RB150/firibastat treatment, subsequently increasing angiotensin 1-7 and activating the MasR while blocking angiotensin III formation, contributes to the antihypertensive effect and the decrease in arginine-vasopressin release induced by RB150/firibastat. firibastat 109-119 glutamyl aminopeptidase Rattus norvegicus 85-88 33683322-7 2021 Our findings suggest that in the brain, the increase in ACE2 activity resulting from APA inhibition by RB150/firibastat treatment, subsequently increasing angiotensin 1-7 and activating the MasR while blocking angiotensin III formation, contributes to the antihypertensive effect and the decrease in arginine-vasopressin release induced by RB150/firibastat. firibastat 340-345 glutamyl aminopeptidase Rattus norvegicus 85-88 33683322-7 2021 Our findings suggest that in the brain, the increase in ACE2 activity resulting from APA inhibition by RB150/firibastat treatment, subsequently increasing angiotensin 1-7 and activating the MasR while blocking angiotensin III formation, contributes to the antihypertensive effect and the decrease in arginine-vasopressin release induced by RB150/firibastat. firibastat 346-356 glutamyl aminopeptidase Rattus norvegicus 85-88