1993
DOI: 10.1097/00005344-199310000-00016
|View full text |Cite
|
Sign up to set email alerts
|

Pharmacology of SC-52458, an Orally Active, Nonpeptide Angiotensin AT1 Receptor Antagonist

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1
1

Citation Types

1
8
0

Year Published

1994
1994
2021
2021

Publication Types

Select...
6
3

Relationship

0
9

Authors

Journals

citations
Cited by 27 publications
(9 citation statements)
references
References 0 publications
1
8
0
Order By: Relevance
“…This finding is also consistent with the findings of an in vitro functional study showing that the Ang II-induced depolarization of the rat superior cervical ganglion was blocked by losartan, but not by PD-123177 (24). In the present in vivo experiment, the ganglionic stimulatory response to Ang II in the dog cardiac sympathetic ganglia was also inhibited by forasartan, which is described as a non-peptide competitive AT1-receptor antagonist (25), but not by PD-123319, an AT2-receptor antagonist. Therefore, the Ang II-induced stimulation of the dog sympathetic ganglia is also mediated by the AT1 subtype of the Ang II receptor.…”
Section: +supporting
confidence: 92%
“…This finding is also consistent with the findings of an in vitro functional study showing that the Ang II-induced depolarization of the rat superior cervical ganglion was blocked by losartan, but not by PD-123177 (24). In the present in vivo experiment, the ganglionic stimulatory response to Ang II in the dog cardiac sympathetic ganglia was also inhibited by forasartan, which is described as a non-peptide competitive AT1-receptor antagonist (25), but not by PD-123319, an AT2-receptor antagonist. Therefore, the Ang II-induced stimulation of the dog sympathetic ganglia is also mediated by the AT1 subtype of the Ang II receptor.…”
Section: +supporting
confidence: 92%
“…The introduction of losartan as the first high-affinity, non-peptide, competitive antagonist with selectivity for A111 receptors has stimulated an extensive research into analogues (Timmermans et al 1993). Compounds such as L-158809 , SR 47436 (Cazaubon et al 1993), SC-52458 (Olins et al 1993), TCV-116 (Inada et al 1994) and ABBOTT-81988 (Lee et al 1994) were more potent than losartan or its metabolite, EXP 3174, and showed promising oral activity. These compounds inhibited AII-induced pressor responses in normotensive rats (Cazaubon et al 1993) and produced long-lasting decreases in blood pressure with minor changes in heart rate in spontaneously hypertensive rats (Olins et al 1993;Inada et al 1994) tensin I1 receptor antagonists did not change blood pressure in DOCA-salt hypertensive rats (Inada et al 1994).…”
Section: Therapeutic Roles Of Selective Angiotensin I1 Receptor Antagmentioning
confidence: 99%
“…These compounds inhibited AII-induced pressor responses in normotensive rats (Cazaubon et al 1993) and produced long-lasting decreases in blood pressure with minor changes in heart rate in spontaneously hypertensive rats (Olins et al 1993;Inada et al 1994) tensin I1 receptor antagonists did not change blood pressure in DOCA-salt hypertensive rats (Inada et al 1994). The antihypertensive responses were additive to ACE inhibitors (Lee et al 1994).…”
Section: Therapeutic Roles Of Selective Angiotensin I1 Receptor Antagmentioning
confidence: 99%
“…Conformational analysis, using the molecular mechanics MM2 method, was carried out for each molecule to obtain the conformational minima within 8 kcal/mol of the global minimum. These minima (about 9000 conformers) were described by 10 interatomic distances that define the relative spatial disposition of five relevant functional groups belonging to all the molecules. A structure-activity relationship between the 3D molecular descriptors and the biological data was then assessed by chemometric techniques; cluster analysis was applied to reduce the large number of conformational minima found for each molecule.…”
Section: Molecular Modelingmentioning
confidence: 99%