PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 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 30882604-0 2019 A pilot double-blind randomized placebo-controlled crossover pharmacodynamic study of the centrally active aminopeptidase A inhibitor, firibastat, in hypertension. firibastat 135-145 glutamyl aminopeptidase Homo sapiens 107-123 30882604-1 2019 OBJECTIVES: We conducted a pilot multicenter double-blind randomized placebo-controlled crossover pharmacodynamic study to evaluate the blood pressure (BP) and the hormonal effects of firibastat, a first-in-class aminopeptidase A inhibitor prodrug, in patients with hypertension. firibastat 184-194 glutamyl aminopeptidase Homo sapiens 213-229 31014072-0 2019 Efficacy and Safety of Firibastat, A First-in-Class Brain Aminopeptidase A Inhibitor, in Hypertensive Overweight Patients of Multiple Ethnic Origins. firibastat 23-33 glutamyl aminopeptidase Homo sapiens 58-74 31014072-16 2019 CONCLUSIONS: Our results demonstrate the efficacy of firibastat in lowering BP in a high-risk diverse population where monotherapy with angiotensin-I converting enzyme inhibitors or angiotensin-II receptor type 1 blockers may be less effective and support the strategy to further investigate firibastat in subjects with difficult-to-treat or potentially resistant hypertension. firibastat 53-63 angiotensin II receptor type 1 Homo sapiens 182-212 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 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 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 30599150-3 2019 We hypothesized that orally administered firibastat (previously named RB150), an APA inhibitor prodrug, would attenuate heart failure (HF) development after MI in mice, by blocking brain RAS hyperactivity. firibastat 41-51 glutamyl aminopeptidase Mus musculus 81-84 30599150-3 2019 We hypothesized that orally administered firibastat (previously named RB150), an APA inhibitor prodrug, would attenuate heart failure (HF) development after MI in mice, by blocking brain RAS hyperactivity. firibastat 70-75 glutamyl aminopeptidase Mus musculus 81-84 30599150-6 2019 Firibastat treatment normalized brain APA hyperactivity, with a return to the control values measured in sham group two weeks after MI. firibastat 0-10 glutamyl aminopeptidase Mus musculus 38-41 30599150-8 2019 Moreover, the mRNA levels of biomarkers of HF (Myh7, Bnp and Anf) were significantly lower following firibastat treatment. firibastat 101-111 myosin, heavy polypeptide 7, cardiac muscle, beta Mus musculus 47-51 30599150-8 2019 Moreover, the mRNA levels of biomarkers of HF (Myh7, Bnp and Anf) were significantly lower following firibastat treatment. firibastat 101-111 natriuretic peptide type B Mus musculus 53-56 30599150-8 2019 Moreover, the mRNA levels of biomarkers of HF (Myh7, Bnp and Anf) were significantly lower following firibastat treatment. firibastat 101-111 natriuretic peptide type A Mus musculus 61-64 30599150-10 2019 Thus, chronic oral firibastat administration after MI in mice prevents cardiac dysfunction by normalizing brain APA hyperactivity, and attenuates cardiac hypertrophy and fibrosis. firibastat 19-29 glutamyl aminopeptidase Mus musculus 112-115 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 28968260-9 2018 Chronic RB150 treatment also significantly decreased plasma arginine vasopressin levels and increased diuresis, which participate to BP decrease by reducing the size of fluid compartment. firibastat 8-13 arginine vasopressin Rattus norvegicus 69-80 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 25474003-6 2014 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 Homo sapiens 61-64 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 24337978-2 2014 QGC001 (originally named RB150) is a prodrug of the specific and selective APA inhibitor EC33, and as such it is the prototype of a new class of centrally acting antihypertensive agents. firibastat 25-30 glutamyl aminopeptidase Homo sapiens 75-78 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 22710644-10 2012 Concomitant oral administration of RB150 with a systemic renin-angiotensin system blocker, enalapril, potentiated the RB150-induced blood pressure decrease achieved in <2 hours. firibastat 35-40 renin Rattus norvegicus 57-62 22710644-10 2012 Concomitant oral administration of RB150 with a systemic renin-angiotensin system blocker, enalapril, potentiated the RB150-induced blood pressure decrease achieved in <2 hours. firibastat 118-123 renin Rattus norvegicus 57-62 22710644-11 2012 Thus, RB150 may be the prototype of a new class of centrally active antihypertensive agents that might be used in combination with classic systemic renin-angiotensin system blockers to improve blood pressure control. firibastat 6-11 renin Rattus norvegicus 148-153 21763394-12 2011 This has led to the development of potent orally active APA inhibitors, such as RB150--the prototype of a new class of centrally acting antihypertensive agents. firibastat 80-85 glutamyl aminopeptidase Homo sapiens 56-59 18175217-5 2008 This led to the development of potent, systematically active APA inhibitors, such as RB150, as a prototype of a new class of centrally acting antihypertensive agents for the treatment of certain forms of hypertension. firibastat 85-90 glutamyl aminopeptidase Homo sapiens 61-64 15748538-5 2005 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 Homo sapiens 61-64 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 15136730-5 2004 We developed RB150, a prodrug of the specific and selective APA inhibitor, EC33. firibastat 13-18 glutamyl aminopeptidase Rattus norvegicus 60-63 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 35163378-9 2022 Firibastat is an antihypertensive drug that affects the brain renin angiotensin system by inhibiting aminopeptidase A. firibastat 0-10 renin Homo sapiens 62-67 34950965-6 2021 This review introduces firibastat as a new therapeutic class of treatment for hypertension focused on the renin angiotensin system in the brain. firibastat 23-33 renin Homo sapiens 106-111 35091008-1 2022 BACKGROUND: Blockade of brain renin-angiotensin system (RAS) overactivity by firibastat, the first centrally acting aminopeptidase A (APA) inhibitor prodrug, has already demonstrated its effectiveness in improving cardiac function after myocardial infarction (MI). firibastat 77-87 glutamyl aminopeptidase Mus musculus 116-132 35091008-1 2022 BACKGROUND: Blockade of brain renin-angiotensin system (RAS) overactivity by firibastat, the first centrally acting aminopeptidase A (APA) inhibitor prodrug, has already demonstrated its effectiveness in improving cardiac function after myocardial infarction (MI). firibastat 77-87 glutamyl aminopeptidase Mus musculus 134-137 35163378-9 2022 Firibastat is an antihypertensive drug that affects the brain renin angiotensin system by inhibiting aminopeptidase A. firibastat 0-10 glutamyl aminopeptidase Homo sapiens 101-117 34020248-7 2021 Interestingly, the chronic administration of a combination of firibastat with [Enalapril+HCTZ] reduced plasma arginine-vasopressin levels by 62% relative to those measured in DOCA-salt rats receiving bitherapy. firibastat 62-72 arginine vasopressin Rattus norvegicus 119-130 33881611-8 2021 We demonstrate that the pharmacological blockade of APA with its selective inhibitor RB150 restores the density of mature spines and significantly reduced filopodia-like processes in hippocampal organotypic slices cultures virally transduced with the Swedish mutated Abeta-precursor protein (betaAPP). firibastat 85-90 glutamyl aminopeptidase Homo sapiens 52-55 33881611-8 2021 We demonstrate that the pharmacological blockade of APA with its selective inhibitor RB150 restores the density of mature spines and significantly reduced filopodia-like processes in hippocampal organotypic slices cultures virally transduced with the Swedish mutated Abeta-precursor protein (betaAPP). firibastat 85-90 amyloid beta (A4) precursor protein Mus musculus 292-299 34020248-0 2021 Effects of firibastat in combination with enalapril and hydrochlorothiazide on blood pressure and vasopressin release in hypertensive DOCA-salt rats. firibastat 11-21 arginine vasopressin Rattus norvegicus 98-109 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 34020248-3 2021 In this study, we evaluated the efficacy of firibastat in combination with enalapril, an angiotensin I-converting enzyme inhibitor, and hydrochlorothiazide (HCTZ), in conscious hypertensive deoxycorticosterone acetate (DOCA)-salt rats, which display high plasma arginine-vasopressin levels, low circulating renin levels and resistance to treatment by systemic RAS blockers. firibastat 44-54 arginine vasopressin Rattus norvegicus 271-282 34020248-8 2021 Our data show that tritherapy with firibastat, enalapril and HCTZ improves BP control and arginine-vasopressin release in an experimental salt-dependent model of hypertension, paving the way for the development of new treatments for patients with currently difficult-to-treat or resistant hypertension. firibastat 35-45 arginine vasopressin Homo sapiens 99-110 34020248-3 2021 In this study, we evaluated the efficacy of firibastat in combination with enalapril, an angiotensin I-converting enzyme inhibitor, and hydrochlorothiazide (HCTZ), in conscious hypertensive deoxycorticosterone acetate (DOCA)-salt rats, which display high plasma arginine-vasopressin levels, low circulating renin levels and resistance to treatment by systemic RAS blockers. firibastat 44-54 renin Rattus norvegicus 307-312 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 arginine vasopressin Rattus norvegicus 66-77 33994025-4 2021 Firibastat, a novel Brain Aminopeptidase inhibitor, may be able to help achieve blood pressure control in those with resistant hypertension. firibastat 0-10 carboxypeptidase Q Homo sapiens 26-40 33683322-0 2021 Brain ACE2 Activation Following Brain Aminopeptidase A Blockade by Firibastat in Salt-dependent Hypertension. firibastat 67-77 angiotensin I converting enzyme 2 Rattus norvegicus 6-10 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 33683322-0 2021 Brain ACE2 Activation Following Brain Aminopeptidase A Blockade by Firibastat in Salt-dependent Hypertension. firibastat 67-77 glutamyl aminopeptidase Rattus norvegicus 38-54 33683322-6 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 angiotensin I converting enzyme 2 Rattus norvegicus 160-164 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 33683322-6 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 angiotensin I converting enzyme 2 Rattus norvegicus 214-218 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 angiotensinogen Rattus norvegicus 15-29 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 MAS1 proto-oncogene like, G protein-coupled receptor Homo sapiens 254-258 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 33683322-3 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 angiotensinogen Rattus norvegicus 15-29 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 60-65 angiotensin I converting enzyme 2 Rattus norvegicus 172-176 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 MAS1 proto-oncogene like, G protein-coupled receptor Homo sapiens 283-287 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 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 arginine vasopressin Rattus norvegicus 66-77 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 angiotensin I converting enzyme 2 Rattus norvegicus 172-176 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 33683322-6 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 angiotensin I converting enzyme 2 Rattus norvegicus 160-164 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 angiotensin I converting enzyme 2 Rattus norvegicus 56-60 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 103-108 MAS1 proto-oncogene like, G protein-coupled receptor Homo sapiens 190-194 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 arginine vasopressin Rattus norvegicus 309-320 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 angiotensin I converting enzyme 2 Rattus norvegicus 56-60 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 109-119 MAS1 proto-oncogene like, G protein-coupled receptor Homo sapiens 190-194 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 arginine vasopressin Rattus norvegicus 309-320 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 angiotensin I converting enzyme 2 Rattus norvegicus 56-60 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 340-345 MAS1 proto-oncogene like, G protein-coupled receptor Homo sapiens 190-194 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 angiotensin I converting enzyme 2 Rattus norvegicus 56-60 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 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 MAS1 proto-oncogene like, G protein-coupled receptor Homo sapiens 190-194 33683322-8 2021 RB150/firibastat treatment constitutes an interesting therapeutic approach to improve BP control in hypertensive patients by inducing in the brain renin-angiotensin system, hyperactivity of the beneficial ACE2/Ang 1-7/MasR axis while decreasing that of the deleterious APA/Ang II/Ang III/ATI receptor axis. firibastat 6-16 angiotensin converting enzyme 2 Homo sapiens 205-209 33683322-8 2021 RB150/firibastat treatment constitutes an interesting therapeutic approach to improve BP control in hypertensive patients by inducing in the brain renin-angiotensin system, hyperactivity of the beneficial ACE2/Ang 1-7/MasR axis while decreasing that of the deleterious APA/Ang II/Ang III/ATI receptor axis. firibastat 6-16 angiopoietin 1 Homo sapiens 210-217 33683322-8 2021 RB150/firibastat treatment constitutes an interesting therapeutic approach to improve BP control in hypertensive patients by inducing in the brain renin-angiotensin system, hyperactivity of the beneficial ACE2/Ang 1-7/MasR axis while decreasing that of the deleterious APA/Ang II/Ang III/ATI receptor axis. firibastat 6-16 MAS1 proto-oncogene like, G protein-coupled receptor Homo sapiens 218-222 33683322-8 2021 RB150/firibastat treatment constitutes an interesting therapeutic approach to improve BP control in hypertensive patients by inducing in the brain renin-angiotensin system, hyperactivity of the beneficial ACE2/Ang 1-7/MasR axis while decreasing that of the deleterious APA/Ang II/Ang III/ATI receptor axis. firibastat 6-16 glutamyl aminopeptidase Homo sapiens 269-272 32955085-3 2020 The oral administration of RB150 renamed firibastat by WHO, an APA inhibitor prodrug, targeting only the S1 subsite, decreases blood pressure in hypertensive patients from various ethnic origins. firibastat 27-32 glutamyl aminopeptidase Homo sapiens 63-66 33520782-0 2021 Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials. firibastat 0-10 glutamyl aminopeptidase Homo sapiens 37-53 33520782-8 2021 Accumulating evidence from preclinical studies demonstrated that the centrally acting APA inhibitor prodrugs (firibastat and NI956) are very safe and effective at reducing blood pressure in various hypertensive animal models. firibastat 110-120 glutamyl aminopeptidase Homo sapiens 86-89 32955085-3 2020 The oral administration of RB150 renamed firibastat by WHO, an APA inhibitor prodrug, targeting only the S1 subsite, decreases blood pressure in hypertensive patients from various ethnic origins. firibastat 41-51 glutamyl aminopeptidase Homo sapiens 63-66 32389345-11 2020 Chronic treatment with oral firibastat (4 or 8 weeks after MI) has been shown to normalize brain APA activity in mice. firibastat 28-38 glutamyl aminopeptidase Mus musculus 97-100 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