PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
14514025-3	2003	In this study, we examined whether vasomotor and respiratory neurons in RVLM participate in above-mentioned responses and whether those neurons respond to direct iontophoretic application of ET-1 and/or an ET-A receptor antagonist, FR139317.	FR 139317	232-240	endothelin receptor type A	Rattus norvegicus	206-210
33279571-7	2021	The decrease in ephrin-A2, -A4, -B2, and -B3 expression by ET-1 treatment was reduced in the presence of BQ788, an ETB receptor antagonist, while FR139317, an ETA receptor antagonist, had no effects.	FR 139317	146-154	endothelin 1	Rattus norvegicus	59-63
18935914-3	2008	An ETA antagonist, FR139317 was used.	FR 139317	19-27	endothelin receptor type A	Rattus norvegicus	3-6
15113846-8	2004	Supply in the drinking water of the ET-1 receptor type A (ETA) antagonist FR139317 [(R-2-[(R)-2-[(S)-2-[[1-(hexahydro-1H-azepinyl)]-carbonyl]amino-4-methylpentanoyl]-amino-3-(2-pyridil)propionic] or mixed ETA/B, but not of selective ETB, antagonists prevented the changes produced by a 21-day treatment with prednisolone.	FR 139317	74-82	endothelin receptor type A	Rattus norvegicus	36-56
15113846-8	2004	Supply in the drinking water of the ET-1 receptor type A (ETA) antagonist FR139317 [(R-2-[(R)-2-[(S)-2-[[1-(hexahydro-1H-azepinyl)]-carbonyl]amino-4-methylpentanoyl]-amino-3-(2-pyridil)propionic] or mixed ETA/B, but not of selective ETB, antagonists prevented the changes produced by a 21-day treatment with prednisolone.	FR 139317	74-82	endothelin receptor type A	Rattus norvegicus	58-61
15113846-8	2004	Supply in the drinking water of the ET-1 receptor type A (ETA) antagonist FR139317 [(R-2-[(R)-2-[(S)-2-[[1-(hexahydro-1H-azepinyl)]-carbonyl]amino-4-methylpentanoyl]-amino-3-(2-pyridil)propionic] or mixed ETA/B, but not of selective ETB, antagonists prevented the changes produced by a 21-day treatment with prednisolone.	FR 139317	74-82	endothelin receptor type A	Rattus norvegicus	205-208
14996949-3	2004	Systemic treatment of mice with the ETA antagonist C33H44N6O5, N-[N-[-N(hexahydro-1H-azepin-1-yl)carbonyl]-L-leucyl]-1-methyl-D-tryptophyl]-3-(2-pyridinyl)-D-alanine (FR139317) inhibited neutrophil accumulation.	FR 139317	167-175	endothelin receptor type A	Mus musculus	36-39
14514025-11	2003	FR139317 did not affect basal activity of the vasomotor neurons but inhibited ET-1-evoked excitation.	FR 139317	0-8	endothelin 1	Rattus norvegicus	78-82
14514025-14	2003	In both cases, FR139317 inhibited the effect of simultaneously applied ET-1.	FR 139317	15-23	endothelin 1	Rattus norvegicus	71-75
12122498-5	2002	The basal MABP of DOCA rats was significantly modified by PAG injections of FR139317, an ETA receptor antagonist, or SB209670, an ETA/ETB receptor antagonist.	FR 139317	76-84	endothelin receptor type A	Rattus norvegicus	89-92
12628441-7	2003	Changes in the above vascular parameters induced by OUA were significantly (p < 0.01) reduced by intra-PAG microinjections of FR139317 (a selective ETA receptor antagonist, 5 nmol), SB209670 (a non-selective ETA/ETB receptor antagonist, 3 nmol), but not by BQ 788 (a selective ETB receptor antagonist, 5 nmol).	FR 139317	129-137	endothelin receptor type A	Rattus norvegicus	151-154
12628441-7	2003	Changes in the above vascular parameters induced by OUA were significantly (p < 0.01) reduced by intra-PAG microinjections of FR139317 (a selective ETA receptor antagonist, 5 nmol), SB209670 (a non-selective ETA/ETB receptor antagonist, 3 nmol), but not by BQ 788 (a selective ETB receptor antagonist, 5 nmol).	FR 139317	129-137	endothelin receptor type A	Rattus norvegicus	211-214
12352314-8	2002	Pretreatment with FR-139317 inhibited the magnitude of ET-1-induced hypertension and increased the duration of the depressor action of ET-1.	FR 139317	18-27	endothelin 1	Rattus norvegicus	55-59
12352314-8	2002	Pretreatment with FR-139317 inhibited the magnitude of ET-1-induced hypertension and increased the duration of the depressor action of ET-1.	FR 139317	18-27	endothelin 1	Rattus norvegicus	135-139
11904527-5	2002	Pretreatment with FR-139317 (ET(A) antagonist, 1 mg/kg) attenuated the pressor and constrictor effects of ET-1 but did not alter responses to IRL-1620.	FR 139317	18-27	endothelin 1	Rattus norvegicus	106-110
11749771-0	2001	Effects of endothelin receptor A antagonist FR139317 on rats with congestive heart failure.	FR 139317	44-52	endothelin receptor type A	Rattus norvegicus	11-32
11698149-5	2001	Intraluminal administration of a selective endothelin B receptor agonist sarafotoxin 6c in precontracted cerebral arteries and in the presence of the endothelin A receptor blocker FR139317 caused vasodilation in a concentration-dependent manner.	FR 139317	180-188	endothelin receptor type A	Rattus norvegicus	150-171
11749771-1	2001	AIM: To study the effects of a selective endothelin receptor A (ETA) antagonist FR139317 on rats with congestive heart failure.	FR 139317	80-88	endothelin receptor type A	Rattus norvegicus	41-62
11749771-1	2001	AIM: To study the effects of a selective endothelin receptor A (ETA) antagonist FR139317 on rats with congestive heart failure.	FR 139317	80-88	endothelin receptor type A	Rattus norvegicus	64-67
11749771-7	2001	RESULTS: Both groups treated with FR139317 (high and low dose) have lower mortality rate (25.0 % and 28.6 % vs 50.0 %) and lower plasma level of ET-1 than that of vehicle [(3.6 +/- 1.2) ng/L and (4.9 +/- 1.5) ng/L vs (5.8 +/- 1.3) ng/L].	FR 139317	34-42	endothelin 1	Rattus norvegicus	145-149
11749771-10	2001	CONCLUSION: Selective ETA antagonist FR139317 improved the hemodynamics and reduced the plasma ET-1 level and the mortality of rats with congestive heart failure	FR 139317	37-45	endothelin receptor type A	Rattus norvegicus	22-25
11749771-10	2001	CONCLUSION: Selective ETA antagonist FR139317 improved the hemodynamics and reduced the plasma ET-1 level and the mortality of rats with congestive heart failure	FR 139317	37-45	endothelin 1	Rattus norvegicus	95-99
11454667-4	2001	The selective ET(A)-receptor antagonist, FR139317, produced parallel rightward shifts of ET-1, S6b and ET-3 concentration-effect curves indicating that the contractions were mediated by ET(A) receptors.	FR 139317	41-49	endothelin 1	Rattus norvegicus	89-93
11477157-10	2001	Continuous administration of FR139317 (50 mg/kg/day) using osmotic minipumps for 3 days significantly attenuated exogenous ET-1-induced decrease in Cin and RBF.	FR 139317	29-37	endothelin 1	Rattus norvegicus	123-127
11359784-6	2001	In addition, the ET(A)-selective antagonist FR139317 inhibited ET-1-induced leptin expression more potently than did the ET(B)-selective antagonist BQ788.	FR 139317	44-52	endothelin receptor type A	Mus musculus	17-22
11359784-6	2001	In addition, the ET(A)-selective antagonist FR139317 inhibited ET-1-induced leptin expression more potently than did the ET(B)-selective antagonist BQ788.	FR 139317	44-52	endothelin 1	Mus musculus	63-67
11454667-4	2001	The selective ET(A)-receptor antagonist, FR139317, produced parallel rightward shifts of ET-1, S6b and ET-3 concentration-effect curves indicating that the contractions were mediated by ET(A) receptors.	FR 139317	41-49	endothelin 3	Rattus norvegicus	103-107
11454667-9	2001	Segments pre-contracted with submaximal concentrations of S6b and ET-3, but not ET-1, rapidly relaxed following wash-out or FR139317 administration.	FR 139317	124-132	endothelin 3	Rattus norvegicus	66-70
11377999-6	2001	The antagonists IRL2500 and FR139317 were used in order to characterise the ET-1-induced response.	FR 139317	28-36	endothelin 1	Rattus norvegicus	76-80
11249854-4	2001	Furthermore, pretreatment of cells with exogenous ET-1 obviously prevented cytochalasin D-elicited activation of MMP-2, an effect that was completely abolished by ET(A) receptor antagonist, FR139317.	FR 139317	190-198	endothelin 1	Rattus norvegicus	50-54
11249854-4	2001	Furthermore, pretreatment of cells with exogenous ET-1 obviously prevented cytochalasin D-elicited activation of MMP-2, an effect that was completely abolished by ET(A) receptor antagonist, FR139317.	FR 139317	190-198	matrix metallopeptidase 2	Rattus norvegicus	113-118
11078369-5	2000	The positive inotropic effect of ET-1 was antagonized by preincubation with FR139317 (10(-6) M).	FR 139317	76-84	endothelin 1	Homo sapiens	33-37
11011035-6	2000	Exogenous endothelin-1 (1-100 nM) did not affect the catecholamine output responses, but it inhibited the responses under treatment with phosphoramidon and FR139317.	FR 139317	156-164	endothelin 1	Rattus norvegicus	10-22
10975592-3	2000	The maximal inhibition induced by ET-1 at 3 x 10(-8) M was approximately 30%, and the median inhibitory (IC50) value of ET-1 was 1.1 x 10(-9) M. The inhibitory action of ET-1 (10(-8) M) on the ISO-induced increase in I(Ca) was markedly attenuated by the ET(A) antagonist FR139317 (10(-6) M) and was partially inhibited by the ET(B) antagonist BQ-788 (10(-6) M).	FR 139317	271-279	endothelin 1	Canis lupus familiaris	120-124
11028503-8	2000	An endothelin type A receptor antagonist, FR139317, negated the inhibitory effect of ET-1 on apoptosis, while the endothelin type B receptor antagonist BQ788 did not show such a negation.	FR 139317	42-50	endothelin 1	Homo sapiens	85-89
11787467-5	2000	Preincubation with the ET(A) receptor antagonist FR139317 (1 microM) decreased significantly (P < 0.005) the potency of ET- I in both atrial and ventricular trabeculae, without any significant changes in Emax (maximum effect obtained with an agonist).	FR 139317	49-57	endothelin receptor type A	Homo sapiens	23-28
10975592-3	2000	The maximal inhibition induced by ET-1 at 3 x 10(-8) M was approximately 30%, and the median inhibitory (IC50) value of ET-1 was 1.1 x 10(-9) M. The inhibitory action of ET-1 (10(-8) M) on the ISO-induced increase in I(Ca) was markedly attenuated by the ET(A) antagonist FR139317 (10(-6) M) and was partially inhibited by the ET(B) antagonist BQ-788 (10(-6) M).	FR 139317	271-279	endothelin 1	Canis lupus familiaris	120-124
10822110-4	2000	The contraction induced by ET-1 was markedly inhibited by BQ123 and FR139317, but BQ788 only slightly inhibited the response induced by ET-1.	FR 139317	68-76	endothelin 1	Homo sapiens	27-31
10822110-7	2000	ET-1 and FR139317 inhibited the specific 125I-ET-1 binding completely, but ET-3, sarafotoxin S6c and BQ3020 only slightly inhibited the specific binding (inhibition, 10-20%), suggesting that ET(A) is the dominant ET receptor subtype in the porcine myometrium.	FR 139317	9-17	endothelin 1	Homo sapiens	46-50
10619182-3	1999	The effect of ET-1 on I(Ca) was abolished by a selective ET(A) receptor antagonist, FR139317 (10(-6) M).	FR 139317	84-92	endothelin-1	Oryctolagus cuniculus	14-18
10696107-6	2000	ET-1 caused a decrease in cyclic AMP in the main pulmonary arteries, an effect that was partially blocked by FR139317 but not influenced by the ET(B)-receptor antagonist BQ-788 (1 microM) or removal of the vascular endothelium.	FR 139317	109-117	endothelin 1	Rattus norvegicus	0-4
10718330-3	2000	We observed an up-regulation of the ET(B) receptor and an amazingly increased sensitivity to ET-1 by 3 log units in pEC50; pEC50(fresh) was 8.7 +/- 0.1, and pEC50(cultured) was 11.7 +/- 0.3. pA2 for FR139317 in the fresh vessel was 7.0 +/- 0.2 whereas it could not be obtained for the cultured vessel, indicating a possible cross-talk between the ET(A) and ET(B) receptors.	FR 139317	199-207	endothelin 1	Rattus norvegicus	93-97
10358117-6	1999	The [Ca2+]i response induced by 1 microM F-180 or dDAVP was selectively blocked by 10 nM of V1a and V2 antagonists (SR 49059 and SR 121463A, respectively).	FR 139317	41-46	arginine vasopressin receptor 1A	Rattus norvegicus	92-95
10528116-9	1999	These findings were supported by laser Doppler flowmetry which determined FR139317 induces reperfusion when injected 10 or 90 min following ET-3.	FR 139317	74-82	endothelin 3	Rattus norvegicus	140-144
10528116-10	1999	ET-3-induced MCA occlusion is therefore amenable to reversal by the ET(A) receptor antagonist FR139317, and this model may offer a means to investigate the neuropathology of reperfusion without the procedure-related artifacts associated with some reperfusion models.	FR 139317	94-102	endothelin 3	Rattus norvegicus	0-4
10340767-6	1999	FR139317, a selective ETA antagonist (23 nmole/day), slightly decreased the number of Vim(+) cells but not that of GFAP(+) cells.	FR 139317	0-8	vimentin	Rattus norvegicus	86-89
10336530-4	1999	The ETA receptor-selective antagonists BQ-123 and FR139317 caused concentration-dependent inhibition of the contractions induced by endothelin-1 and sarafotoxin S6b, but both antagonists were significantly less potent in inhibiting contractions induced by endothelin-1 than sarafotoxin S6b.	FR 139317	50-58	endothelin-1 receptor	Ovis aries	4-7
10336530-4	1999	The ETA receptor-selective antagonists BQ-123 and FR139317 caused concentration-dependent inhibition of the contractions induced by endothelin-1 and sarafotoxin S6b, but both antagonists were significantly less potent in inhibiting contractions induced by endothelin-1 than sarafotoxin S6b.	FR 139317	50-58	EDN1	Ovis aries	132-144
10336530-4	1999	The ETA receptor-selective antagonists BQ-123 and FR139317 caused concentration-dependent inhibition of the contractions induced by endothelin-1 and sarafotoxin S6b, but both antagonists were significantly less potent in inhibiting contractions induced by endothelin-1 than sarafotoxin S6b.	FR 139317	50-58	EDN1	Ovis aries	256-268
10340767-6	1999	FR139317, a selective ETA antagonist (23 nmole/day), slightly decreased the number of Vim(+) cells but not that of GFAP(+) cells.	FR 139317	0-8	endothelin receptor type A	Rattus norvegicus	22-25
9605569-9	1998	The ET(A) receptor antagonist FR 139317 (1 microM) had no effect on the potency of ET-1 in any vessel studied but abolished the increased response to ET-1 in the chronically hypoxic vessels.	FR 139317	30-39	endothelin 1	Rattus norvegicus	150-154
10465357-2	1999	The increases in blood pressure induced by ANGII (1 nmol; 37 +/- 4 mmHg, n=5) were greatly reduced (>85%) by pre-administration of the ET(A) receptor antagonist FR139317 (5 nmol/rat) to the PAG area, but were unaffected by the ET(B) receptor antagonist BQ-788 (5 nmol/rat).	FR 139317	164-172	angiotensinogen	Rattus norvegicus	43-48
9826221-5	1998	FR139317-induced osteopenia was associated with a significant decrease in the serum osteocalcin concentration but no change in the urinary excretion of pyridinium cross-links of collagen.	FR 139317	0-8	bone gamma-carboxyglutamate protein	Rattus norvegicus	84-95
9781938-5	1998	Treatment with 100 nM dexamethasone for 24 h reduced the peak increase of intracellular free Ca2+ induced by ET-1 (100 nM) by 50%, an effect that was dose-dependently inhibited by the specific ET(A)-receptor antagonist FR139317.	FR 139317	219-227	endothelin 1	Rattus norvegicus	109-113
9720787-11	1998	FR139317 inhibited responses to ET-1 in vessels from 0-24 h and 4 day, but not fetal, rabbits (pKb: 6.4 in 4 day rabbits).	FR 139317	0-8	endothelin-1	Oryctolagus cuniculus	32-36
9539881-12	1998	In fresh mesenteric arterial segments FR139317 (ETA receptor antagonist) and bosentan (ETA/ETB receptor antagonist) but not IRL 2500 (ETB receptor antagonist) shifted the ET-1-induced concentration-response curve in parallel to the right.	FR 139317	38-46	endothelin receptor type A	Rattus norvegicus	48-51
9595434-7	1998	The attenuating effect of ET-1 was completely blocked by 1 microM FR139317, suggesting that the effect is primarily mediated by the ETA receptor.	FR 139317	66-74	endothelin 1	Homo sapiens	26-30
9595415-5	1998	The ETA receptor antagonist FR139317 partially blocked this ET-1-mediated inhibition of cAMP accumulation in the main extralobar artery.	FR 139317	28-36	endothelin 1	Rattus norvegicus	60-64
9595540-5	1998	The increases in SAPP caused by injection of ET-1 (ETA/ETB agonist) were markedly reduced in the presence of the selective ETA antagonist FR-139317, whereas those induced by IRL-1620 (an ETB agonist) and norepinephrine (NE) were unchanged.	FR 139317	138-147	endothelin 1	Homo sapiens	45-49
9595540-5	1998	The increases in SAPP caused by injection of ET-1 (ETA/ETB agonist) were markedly reduced in the presence of the selective ETA antagonist FR-139317, whereas those induced by IRL-1620 (an ETB agonist) and norepinephrine (NE) were unchanged.	FR 139317	138-147	endothelin receptor type A	Homo sapiens	51-54
9595540-5	1998	The increases in SAPP caused by injection of ET-1 (ETA/ETB agonist) were markedly reduced in the presence of the selective ETA antagonist FR-139317, whereas those induced by IRL-1620 (an ETB agonist) and norepinephrine (NE) were unchanged.	FR 139317	138-147	endothelin receptor type B	Homo sapiens	55-58
9595540-5	1998	The increases in SAPP caused by injection of ET-1 (ETA/ETB agonist) were markedly reduced in the presence of the selective ETA antagonist FR-139317, whereas those induced by IRL-1620 (an ETB agonist) and norepinephrine (NE) were unchanged.	FR 139317	138-147	endothelin receptor type A	Homo sapiens	123-126
9595410-6	1998	Pretreatment with the ETA antagonist FR139317 and the ETB antagonist BQ788 inhibited CPR increases with ET-1 infusion.	FR 139317	37-45	endothelin receptor type A	Rattus norvegicus	22-25
9595410-6	1998	Pretreatment with the ETA antagonist FR139317 and the ETB antagonist BQ788 inhibited CPR increases with ET-1 infusion.	FR 139317	37-45	endothelin 1	Rattus norvegicus	104-108
9595410-7	1998	However, vasoconstrictor responses to ET-1 were still greater in SHR than in WKY after FR139317 or BQ788 infusion.	FR 139317	87-95	endothelin 1	Rattus norvegicus	38-42
9595417-2	1998	Perfusion of the arteries with a subpressor dose of ET-1 (3 x 10(-10) M) for 15 min markedly enhanced the pressor responses to NE (10(-6) and 3 x 10(-6) M), and this effect was significantly prevented by BQ788 (10(-6) M) but not by FR139317 (10(-6) M).	FR 139317	232-240	endothelin 1	Rattus norvegicus	52-56
9553399-15	1998	Endothelin- converting enzyme inhibitor (phosphoramidon) and ET-A/B r antagonists (bosentan, BQ-123, FR139317) may have potential role as vasodilators in the treatment of hypertension.	FR 139317	101-109	endothelin receptor type A	Homo sapiens	61-67
9242182-9	1997	The effect of ET-1 appeared to be mediated by an ETA receptor, because it was prevented by FR139317, an ETA-selective antagonist (1 mumol/L, n = 4), and sarafotoxin s6c, an ETB-selective agonist (100 nmol/L, n = 4), could not inhibit the ISO-enhanced IK.	FR 139317	91-99	endothelin-1	Cavia porcellus	14-18
9298531-5	1997	Intravenous injection of a selective ETA receptor antagonist, FR139317 (0.5 mumol kg-1, for 20 min) induced a very small fall in blood pressure.	FR 139317	62-70	endothelin receptor type A	Rattus norvegicus	37-40
9154335-8	1997	This agonist profile, together with the findings that the ETA receptor-selective antagonists, BQ-123 and FR-139317 caused concentration-dependent, rightward shifts of the concentration-effect curves to each agonist indicated that ET-1-induced contractions in rat renal artery were mediated via ETA receptors.	FR 139317	105-114	endothelin receptor type A	Rattus norvegicus	58-61
9154335-8	1997	This agonist profile, together with the findings that the ETA receptor-selective antagonists, BQ-123 and FR-139317 caused concentration-dependent, rightward shifts of the concentration-effect curves to each agonist indicated that ET-1-induced contractions in rat renal artery were mediated via ETA receptors.	FR 139317	105-114	endothelin receptor type A	Rattus norvegicus	294-297
9154335-10	1997	BQ-123 and FR-139317 were both significantly more potent inhibitors of contractions induced by StxS6b or ET-3 than of responses to ET-1, raising the possibility that a component of ET-1-induced contraction was mediated through atypical, BQ-123 (or FR-139317)-insensitive ETA receptors.	FR 139317	11-20	endothelin receptor type A	Rattus norvegicus	271-274
9440503-8	1997	The functional effects of ET-1 were completely inhibited by the ET(A)-selective antagonists FR139317 and A-127722, suggesting that the effects were mediated by the ET(A) receptor.	FR 139317	92-100	endothelin 1	Homo sapiens	26-30
9175058-3	1997	This study was designed to assess whether the glomerular expression of mRNA for ECM components, ET-1, metalloproteinases (MMP), and a tissue inhibitor of metalloproteinases (TIMP) is modulated by a specific endothelin receptor A antagonist (FR139317) or angiotensin-converting enzyme inhibitor (enalapril) in PAN-injected rats.	FR 139317	241-249	TIMP metallopeptidase inhibitor 1	Rattus norvegicus	174-178
9175058-14	1997	Both enalapril and FR139317 attenuated the increases in mRNA levels for alpha 1 (IV) collagen chain (P < 0.01), laminin chains (P < 0.01), and ET-1 (P < 0.01), and attenuated the decreases in mRNA levels for HSPG (P < 0.01) in glomeruli of PAN-injected rats.	FR 139317	19-27	endothelin 1	Rattus norvegicus	149-153
9175058-14	1997	Both enalapril and FR139317 attenuated the increases in mRNA levels for alpha 1 (IV) collagen chain (P < 0.01), laminin chains (P < 0.01), and ET-1 (P < 0.01), and attenuated the decreases in mRNA levels for HSPG (P < 0.01) in glomeruli of PAN-injected rats.	FR 139317	19-27	syndecan 2	Rattus norvegicus	217-221
9175058-16	1997	CONCLUSIONS: These data suggest that the beneficial effects of enalapril and FR139317 may be related to modulation of glomerular mRNA expression of ECM components and ET-1 and that these agents may follow a different mechanism in regulating the glomerular mRNA expression for MMP-2 and TIMP-1 in PAN nephrosis.	FR 139317	77-85	endothelin 1	Rattus norvegicus	167-171
9175058-16	1997	CONCLUSIONS: These data suggest that the beneficial effects of enalapril and FR139317 may be related to modulation of glomerular mRNA expression of ECM components and ET-1 and that these agents may follow a different mechanism in regulating the glomerular mRNA expression for MMP-2 and TIMP-1 in PAN nephrosis.	FR 139317	77-85	matrix metallopeptidase 2	Rattus norvegicus	276-281
9175058-16	1997	CONCLUSIONS: These data suggest that the beneficial effects of enalapril and FR139317 may be related to modulation of glomerular mRNA expression of ECM components and ET-1 and that these agents may follow a different mechanism in regulating the glomerular mRNA expression for MMP-2 and TIMP-1 in PAN nephrosis.	FR 139317	77-85	TIMP metallopeptidase inhibitor 1	Rattus norvegicus	286-292
8930216-5	1996	Enhancement of K+ current was inhibited by FR139317 (an ET(A) receptor antagonist) and by buffering intracellular Ca+2, which suggests that ET(A) receptor stimulation also activates Ca(+2)-activated K+ channels.	FR 139317	43-51	endothelin receptor type A	Rattus norvegicus	56-61
8930216-5	1996	Enhancement of K+ current was inhibited by FR139317 (an ET(A) receptor antagonist) and by buffering intracellular Ca+2, which suggests that ET(A) receptor stimulation also activates Ca(+2)-activated K+ channels.	FR 139317	43-51	endothelin receptor type A	Rattus norvegicus	140-145
8800365-5	1996	FR 139317 was a more potent antagonist of contractions induced by endothelin-3 than the other peptides.	FR 139317	0-9	endothelin 3	Homo sapiens	66-78
8843784-3	1996	An ETA-selective antagonist, FR139317, inhibited 0.2 nM ET-1-induced DNA synthesis dose dependently, showing complete inhibition at 1 microM.	FR 139317	29-37	endothelin receptor type A	Homo sapiens	3-6
8769122-3	1996	Delivery of the ETA receptor antagonist, FR139317, 5 min prior to giving endothelin-1 greatly potentiated these changes.	FR 139317	41-49	endothelin-1	Cavia porcellus	73-85
8701880-5	1996	Groups A and C received saline infusions; group B received continuous infusions of the ETA-selective antagonist FR139317.	FR 139317	112-120	endothelin receptor type A	Canis lupus familiaris	87-90
8701880-7	1996	Administration of the ETA antagonist FR139317 did not alter infarct size.	FR 139317	37-45	endothelin receptor type A	Canis lupus familiaris	22-25
8854203-1	1996	By using BQ-788 as a selective endothelin ETB-receptor antagonist and FR139317 as a selective endothelin ETA-receptor antagonist, we have characterized the receptor subtypes mediating the systemic and renal vascular effects of endothelin-1 and IRL1620, a selective endothelin ETB-receptor agonist (succinyl-[Glu9,Ala11,5]-endothelin-1(8-21)), in anesthetized rats.	FR 139317	70-78	endothelin 1	Rattus norvegicus	227-239
8613968-4	1996	The selective ET(A) antagonist FR139317 effectively antagonized the PIE of ET-3.	FR 139317	31-39	endothelin-3	Oryctolagus cuniculus	75-79
8613968-9	1996	Thus, in the presence of FR139317, the PIEs of ET-3 and ET-1 were partially dissociated from the PI hydrolysis that was induced by these isopeptides.	FR 139317	25-33	endothelin-3	Oryctolagus cuniculus	47-51
8680707-2	1995	Preinjection (10 min before) of FR 139317 (an ETA receptor selective antagonist; 5 nmol) or SB 209670 (an ETA/ETB receptor non-selective antagonist; 5 nmol) to the PAG reduced the pressor response to NMDA whereas BQ-788 (an ETB receptor selective antagonist; 5 nmol) did not affect the NMDA-induced hypertension.	FR 139317	32-41	endothelin receptor type A	Rattus norvegicus	46-49
8613968-9	1996	Thus, in the presence of FR139317, the PIEs of ET-3 and ET-1 were partially dissociated from the PI hydrolysis that was induced by these isopeptides.	FR 139317	25-33	endothelin-1	Oryctolagus cuniculus	56-60
8613968-10	1996	FR139317 inhibited the specific binding of [125I]ET-1 and of [125I]ET-3, and it was apparent that FR139317 had a high-affinity and a low-affinity site for competing for specific binding with each ligand.	FR 139317	0-8	endothelin-1	Oryctolagus cuniculus	49-53
8613968-10	1996	FR139317 inhibited the specific binding of [125I]ET-1 and of [125I]ET-3, and it was apparent that FR139317 had a high-affinity and a low-affinity site for competing for specific binding with each ligand.	FR 139317	0-8	endothelin-3	Oryctolagus cuniculus	67-71
8636441-8	1996	Acute endothelin A receptor blockade with FR-139317 resulted in significant decreases in mean arterial pressure and systemic vascular resistance in TIVCC.	FR 139317	42-51	endothelin receptor type A	Canis lupus familiaris	6-27
8632419-3	1996	The pseudotetrapeptide FR-139317 is a potent and highly selective antagonist of the endothelin-A (ET(A)) receptor; however, its peptidic nature leads to poor oral absorption characteristics which make it an unlikely drug candidate.	FR 139317	23-32	endothelin receptor type A	Homo sapiens	84-96
8632419-3	1996	The pseudotetrapeptide FR-139317 is a potent and highly selective antagonist of the endothelin-A (ET(A)) receptor; however, its peptidic nature leads to poor oral absorption characteristics which make it an unlikely drug candidate.	FR 139317	23-32	endothelin receptor type A	Homo sapiens	98-103
8821534-4	1996	The linear tripeptide antagonist, FR139317 competed for [125I]-ET-1 binding to human left ventricle with over 200,000 fold selectivity for the ETA receptor (KD ETA = 1.20 +/- 0.28 nM, KDETB = 287 +/- 93 microM).	FR 139317	34-42	endothelin receptor type A	Homo sapiens	143-146
8821534-4	1996	The linear tripeptide antagonist, FR139317 competed for [125I]-ET-1 binding to human left ventricle with over 200,000 fold selectivity for the ETA receptor (KD ETA = 1.20 +/- 0.28 nM, KDETB = 287 +/- 93 microM).	FR 139317	34-42	endothelin receptor type A	Homo sapiens	160-163
8821534-15	1996	The results show that the ETA antagonists, BQ123 and FR139317, are highly selective for ETA receptors in all cardiac tissues tested, whereas BQ788 has a low affinity and no selectivity in this human tissue.	FR 139317	53-61	endothelin receptor type A	Homo sapiens	26-29
8821534-15	1996	The results show that the ETA antagonists, BQ123 and FR139317, are highly selective for ETA receptors in all cardiac tissues tested, whereas BQ788 has a low affinity and no selectivity in this human tissue.	FR 139317	53-61	endothelin receptor type A	Homo sapiens	88-91
8959749-7	1996	The potency of FR 139317 was 20-fold higher to antagonize ET-3 than ET-1, and threefold higher to block ET-2 than ET-1.	FR 139317	15-24	endothelin 3	Rattus norvegicus	58-62
8959749-7	1996	The potency of FR 139317 was 20-fold higher to antagonize ET-3 than ET-1, and threefold higher to block ET-2 than ET-1.	FR 139317	15-24	endothelin 1	Rattus norvegicus	68-72
8959749-7	1996	The potency of FR 139317 was 20-fold higher to antagonize ET-3 than ET-1, and threefold higher to block ET-2 than ET-1.	FR 139317	15-24	endothelin 2	Rattus norvegicus	104-108
8959749-7	1996	The potency of FR 139317 was 20-fold higher to antagonize ET-3 than ET-1, and threefold higher to block ET-2 than ET-1.	FR 139317	15-24	endothelin 1	Rattus norvegicus	114-118
8680707-2	1995	Preinjection (10 min before) of FR 139317 (an ETA receptor selective antagonist; 5 nmol) or SB 209670 (an ETA/ETB receptor non-selective antagonist; 5 nmol) to the PAG reduced the pressor response to NMDA whereas BQ-788 (an ETB receptor selective antagonist; 5 nmol) did not affect the NMDA-induced hypertension.	FR 139317	32-41	endothelin receptor type B	Rattus norvegicus	224-227
7490151-3	1995	We conducted the present study to determine whether the specific endothelin type A (ETA) receptor antagonist FR 139317 prevents cyclosporine-induced hypertension and whether cyclosporine increases ETA receptor mRNA in blood vessels.	FR 139317	109-118	endothelin receptor type A	Rattus norvegicus	84-87
7586319-5	1995	In group 2 dogs (n = 5), the same dose of ET-1 was infused with 4 micrograms/kg per minute of the specific ET-A receptor antagonist FR-139317.	FR 139317	132-141	endothelin receptor type A	Canis lupus familiaris	107-111
7586319-14	1995	CONCLUSIONS: The present study demonstrates that low concentrations of exogenous ET-1, which may mimic pathophysiological concentrations, result in coronary vasoconstriction mediated predominantly via the ET-A receptor because such vasoconstriction is significantly attenuated by blockade with FR-139317.	FR 139317	294-303	endothelin 1	Canis lupus familiaris	81-85
7586319-14	1995	CONCLUSIONS: The present study demonstrates that low concentrations of exogenous ET-1, which may mimic pathophysiological concentrations, result in coronary vasoconstriction mediated predominantly via the ET-A receptor because such vasoconstriction is significantly attenuated by blockade with FR-139317.	FR 139317	294-303	endothelin receptor type A	Canis lupus familiaris	205-209
7490151-10	1995	The specific ETA receptor antagonist FR 139317 may prevent the hypertension induced by cyclosporine.	FR 139317	37-46	endothelin receptor type A	Rattus norvegicus	13-16
7788905-6	1995	In PH beagles, ET-1 infusion increased SAP, which was attenuated by FR139317 (an endothelin type [ET] A receptor antagonist), and produced a dose-dependent decrease in PAP, which was attenuated by RES-701-1 (an ETB receptor antagonist).	FR 139317	68-76	endothelin 1	Homo sapiens	15-19
8549645-5	1995	Furthermore, pretreatment of brown adipocytes with endothelin ETA receptor antagonist FR139317 antagonized the endothelin-1-induced reduction of lipoprotein lipase activity and lipoprotein lipase mRNA.	FR 139317	86-94	endothelin 1	Homo sapiens	111-123
8549645-5	1995	Furthermore, pretreatment of brown adipocytes with endothelin ETA receptor antagonist FR139317 antagonized the endothelin-1-induced reduction of lipoprotein lipase activity and lipoprotein lipase mRNA.	FR 139317	86-94	lipoprotein lipase	Homo sapiens	145-163
8549645-5	1995	Furthermore, pretreatment of brown adipocytes with endothelin ETA receptor antagonist FR139317 antagonized the endothelin-1-induced reduction of lipoprotein lipase activity and lipoprotein lipase mRNA.	FR 139317	86-94	lipoprotein lipase	Homo sapiens	177-195
7560748-6	1995	The hyperventilation evoked by ET-1 was antagonised by the ETA receptor antagonist FR139317, but responses to hypoxia (10% oxygen) and to cyanide were unaffected.	FR 139317	83-91	endothelin 1	Rattus norvegicus	31-35
7762634-4	1995	FR-139317 and BQ-123, two ETA antagonists, both inhibited 125I-ET-1 binding.	FR 139317	0-9	endothelin receptor type A	Homo sapiens	26-29
7670725-10	1995	The ETA receptor-selective antagonist, FR 139317 (2.5 mg kg-1) inhibited the ET-1 (1 nmol kg-1)-induced pressor response, haemoconcentration and albumin extravasation by 75, 77 and 60-70%, respectively, whereas it did not attenuate IRL 1620 (1 nmol kg-1)-induced changes.	FR 139317	39-48	endothelin-1	Cavia porcellus	77-81
7647976-16	1995	ET-1-induced vasoconstriction was blocked by the ETA-selective antagonists, BQ123 and FR139317.	FR 139317	86-94	endothelin 1	Homo sapiens	0-4
7774661-4	1995	The contractile response to endothelin-1 of adult but not neonatal duodenum was significantly antagonized by pretreatment with FR139317 (1 microM), an endothelin ETA receptor antagonist.	FR 139317	127-135	endothelin 1	Rattus norvegicus	28-40
7723234-1	1995	The present study was designed to assess whether a specific endothelin A (ETA) receptor antagonist, FR139317, affects the progression of lupus nephritis and affects transcription of mRNA for extracellular matrix (ECM) components, metalloproteinases (MMPs) and tissue inhibitor of metalloproteinase (TIMP)-1, and accumulation of ECM proteins in the renal cortex of NZB/W F1 mice.	FR 139317	100-108	endothelin receptor type A	Mus musculus	60-87
7723234-1	1995	The present study was designed to assess whether a specific endothelin A (ETA) receptor antagonist, FR139317, affects the progression of lupus nephritis and affects transcription of mRNA for extracellular matrix (ECM) components, metalloproteinases (MMPs) and tissue inhibitor of metalloproteinase (TIMP)-1, and accumulation of ECM proteins in the renal cortex of NZB/W F1 mice.	FR 139317	100-108	matrix metallopeptidase 13	Mus musculus	250-254
7723234-1	1995	The present study was designed to assess whether a specific endothelin A (ETA) receptor antagonist, FR139317, affects the progression of lupus nephritis and affects transcription of mRNA for extracellular matrix (ECM) components, metalloproteinases (MMPs) and tissue inhibitor of metalloproteinase (TIMP)-1, and accumulation of ECM proteins in the renal cortex of NZB/W F1 mice.	FR 139317	100-108	tissue inhibitor of metalloproteinase 1	Mus musculus	260-306
7723234-1	1995	The present study was designed to assess whether a specific endothelin A (ETA) receptor antagonist, FR139317, affects the progression of lupus nephritis and affects transcription of mRNA for extracellular matrix (ECM) components, metalloproteinases (MMPs) and tissue inhibitor of metalloproteinase (TIMP)-1, and accumulation of ECM proteins in the renal cortex of NZB/W F1 mice.	FR 139317	100-108	TP53 regulated inhibitor of apoptosis 1	Mus musculus	364-372
7881728-12	1995	The ETA-selective ligand FR139317 competed for [125I]-PD151242 binding in human left ventricle with nanomolar affinity (KD = 0.37 +/- 0.10 nM), whereas the ETB-selective compound, BQ3020, competed with only micromolar affinity (KD = 1.5 +/- 0.26 microM).	FR 139317	25-33	endothelin receptor type B	Homo sapiens	156-159
8587363-7	1995	Infusion of the ETA receptor antagonist FR-139317 (0.3 microM) markedly reduced both ET-1- and S6b-induced vasoconstriction without affecting that evoked by NE.	FR 139317	40-49	endothelin receptor type A	Canis lupus familiaris	16-19
8587411-6	1995	These changes persisted after coincubation with both ET-1 and FR139317, indicating that the antagonist was able to block the effects of exogenous ET-1.	FR 139317	62-70	endothelin 1	Homo sapiens	146-150
8587446-8	1995	injections of the ETA inhibitor FR139317, 32 mg/kg.	FR 139317	32-40	endothelin receptor type A	Rattus norvegicus	18-21
8587363-7	1995	Infusion of the ETA receptor antagonist FR-139317 (0.3 microM) markedly reduced both ET-1- and S6b-induced vasoconstriction without affecting that evoked by NE.	FR 139317	40-49	endothelin 1	Canis lupus familiaris	85-89
8904028-7	1995	Moreover, these contractility response rates were significantly reduced (32.8 +/- 21.0%) with the addition of the ET-1 receptor antagonist FR139317.	FR 139317	139-147	endothelin-1	Sus scrofa	114-118
7549229-6	1994	The contraction evoked by endothelin-1 is mediated via an EtA-receptor subtype since the EtA-receptor antagonist FR139317 attenuated the response.	FR 139317	113-121	endothelin 1	Bos taurus	26-38
7965709-5	1994	Intrathecal injection of ET-1 depressed the phase 1 and 2 flinching behavior in a dose-dependent manner and this ET-1 effect was antagonized by FR139317.	FR 139317	144-152	endothelin 1	Homo sapiens	25-29
7965709-5	1994	Intrathecal injection of ET-1 depressed the phase 1 and 2 flinching behavior in a dose-dependent manner and this ET-1 effect was antagonized by FR139317.	FR 139317	144-152	endothelin 1	Homo sapiens	113-117
7516007-5	1994	FR 139317, a selective ETA receptor antagonist, significantly decreased the potency of ET-1 and ET-2 responses in both human coronary arteries and veins, but the maximum effect obtained did not change significantly.	FR 139317	0-9	endothelin 1	Homo sapiens	87-91
7862251-0	1994	FR139317, a specific ETA-receptor antagonist, inhibits cerebral activation by intraventricular endothelin-1 in conscious rats.	FR 139317	0-8	endothelin 1	Rattus norvegicus	95-107
7836667-3	1994	The selective ETA receptor antagonist FR 139317 mediated a shift to the right of the concentration-response curve of ET-1.	FR 139317	38-47	endothelin 1	Homo sapiens	117-121
7921626-16	1994	The selective ETA receptor antagonist, FR 139317 (2.5 mg kg-1) significantly blunted the pressor action of ET-1 and the accompanying bradycardia without affecting the depressor response.	FR 139317	39-48	endothelin 1	Rattus norvegicus	107-111
8075866-0	1994	Effects of an ET1-receptor antagonist, FR139317, on regional haemodynamic responses to endothelin-1 and [Ala11,15]Ac-endothelin-1 (6-21) in conscious rats.	FR 139317	39-47	endothelin 1	Rattus norvegicus	87-99
8075866-0	1994	Effects of an ET1-receptor antagonist, FR139317, on regional haemodynamic responses to endothelin-1 and [Ala11,15]Ac-endothelin-1 (6-21) in conscious rats.	FR 139317	39-47	endothelin 1	Rattus norvegicus	117-129
8075866-15	1994	However, in the presence of FR139317, significant pressor and renal, mesenteric and hindquarters vasoconstrictor responses to ET-1 and BQ-3020 still occurred, and the initial depressor and hindquarters vasodilator responses to both peptides were unchanged.	FR 139317	28-36	endothelin 1	Rattus norvegicus	126-130
8032665-7	1994	Infusion of FR 139317 (1 microM) significantly attenuated the increase in CPP caused by ET-1 (30 pmol: 3 +/- 1 mmHg, 100 pmol: 8 +/- 2 mmHg; n = 8).	FR 139317	12-21	endothelin-1	Oryctolagus cuniculus	88-92
7516007-5	1994	FR 139317, a selective ETA receptor antagonist, significantly decreased the potency of ET-1 and ET-2 responses in both human coronary arteries and veins, but the maximum effect obtained did not change significantly.	FR 139317	0-9	endothelin 2	Homo sapiens	96-100
7516007-7	1994	The effect of the selective ETA receptor antagonist FR 139317 indicates that the contraction induced by ET-1 and ET-2 in both arteries and veins is mediated by ETA receptors.	FR 139317	52-61	endothelin 1	Homo sapiens	104-108
7516007-7	1994	The effect of the selective ETA receptor antagonist FR 139317 indicates that the contraction induced by ET-1 and ET-2 in both arteries and veins is mediated by ETA receptors.	FR 139317	52-61	endothelin 2	Homo sapiens	113-117
8258520-10	1993	The endothelinA receptor antagonist FR-139317 significantly reduced vasoconstriction to ET-1 (10(-10) M; P < 0.001 versus control).	FR 139317	36-45	endothelin 1	Homo sapiens	88-92
8124808-6	1994	Moreover, the ETB receptor agonist sarafotoxin S6c induced contraction in vessels preincubated with FR139317.	FR 139317	100-108	endothelin receptor type B	Homo sapiens	14-17
8004396-6	1994	The ETA receptor selective antagonists, BQ-123 and FR 139317, both partially blocked the increase in perfusion pressure induced by ET-1.	FR 139317	51-60	endothelin receptor type A	Rattus norvegicus	4-7
8004396-6	1994	The ETA receptor selective antagonists, BQ-123 and FR 139317, both partially blocked the increase in perfusion pressure induced by ET-1.	FR 139317	51-60	endothelin 1	Rattus norvegicus	131-135
8135123-8	1994	The new specific competitive ETA receptor antagonist, FR 139317, abolished the vasoconstrictor response to both endothelin-2 and endothelin-3 in vivo, whereas the preceding vasodilator responses were unaffected.	FR 139317	54-63	endothelin 2	Homo sapiens	112-124
8135123-8	1994	The new specific competitive ETA receptor antagonist, FR 139317, abolished the vasoconstrictor response to both endothelin-2 and endothelin-3 in vivo, whereas the preceding vasodilator responses were unaffected.	FR 139317	54-63	endothelin 3	Homo sapiens	129-141
8377387-2	1993	Here we evaluated whether a specific endothelin subtype A (ETA) receptor antagonist, FR139317, reduced signs of disease activity in this model.	FR 139317	85-93	endothelin receptor type A	Rattus norvegicus	59-62
8243552-0	1993	Comparative effects of the two endothelin ETA receptor antagonists, BQ-123 and FR139317, on endothelin-1-induced contraction in guinea-pig iliac artery.	FR 139317	79-87	endothelin-1	Cavia porcellus	92-104
8243552-5	1993	Both FR139317 (1-10 microM) and BQ-123 (0.1-1 microM) surmountably antagonized the effects of endothelin-1.	FR 139317	5-13	endothelin-1	Cavia porcellus	94-106
8243544-1	1993	Incomplete inhibition of endothelin-1-induced pressor effects by FR-139317, a novel, potent, ETA receptor antagonist, was observed in conscious, normotensive rats.	FR 139317	65-74	endothelin 1	Rattus norvegicus	25-37
8243544-2	1993	Maximum inhibition by FR-139317 of the endothelin-1 pressor response (0.1, 0.3, 1.0 nmol/kg) was 49 +/- 7, 41 +/- 3, 62 +/- 5%, respectively.	FR 139317	22-31	endothelin 1	Rattus norvegicus	39-51
8358553-6	1993	Intravenous infusion of FR139317 at 0.2 (n = 4) or 0.6 mg kg-1 min-1 (n = 4) inhibited the ET-1 pressor response by 83 or 89%, respectively.	FR 139317	24-32	endothelin-1	Oryctolagus cuniculus	91-95
8213182-10	1993	The new specific competitive ETA receptor antagonist FR 139317 was found to be fully effective in vivo, insofar as it abolished the constrictor response to endothelin-1.	FR 139317	53-62	endothelin receptor type A	Homo sapiens	29-32
8213182-10	1993	The new specific competitive ETA receptor antagonist FR 139317 was found to be fully effective in vivo, insofar as it abolished the constrictor response to endothelin-1.	FR 139317	53-62	endothelin 1	Homo sapiens	156-168
8358553-9	1993	The transient depressor response (-16 +/- 3 mmHg) which preceded the rise in blood pressure induced by ET-1 (1 nmol kg-1, i.a., n = 8) was enhanced by an intravenous infusion of FR139317 (0.6 mg kg-1 min-1) to -35 +/- 5 mmHg (P < 0.05, n = 4).	FR 139317	178-186	endothelin-1	Oryctolagus cuniculus	103-107
7509926-5	1993	Force evoked by ET-1 was minimally affected by the relatively ETA-selective (in comparison with ETB) receptor antagonists BQ-123 and FR139317.	FR 139317	133-141	endothelin-1	Oryctolagus cuniculus	16-20
1366258-0	1992	Inhibition of endothelin (ET-1) induced pressor responses by the endothelin (ETA) receptor antagonist FR139317 in the pithed rat.	FR 139317	102-110	endothelin receptor type A	Rattus norvegicus	77-80
1366258-7	1992	We conclude that FR139317 in the pithed rat potently inhibits ET-1 mediated pressor responses and that this agent may become a significant tool to elucidate the putative physiological and pathophysiological role of ETA receptor mediated responses.	FR 139317	17-25	endothelin receptor type A	Rattus norvegicus	215-218