Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C31H32N4O3 |
| Molecular Weight | 508.6108 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C1=C(C)C=C(CN2C=NC3=C2CC(N(C3)C(=O)C(C4=CC=CC=C4)C5=CC=CC=C5)C(O)=O)C=C1
InChI
InChIKey=YSTVFDAKLDMYCR-UHFFFAOYSA-N
InChI=1S/C31H32N4O3/c1-21-16-22(14-15-26(21)33(2)3)18-34-20-32-25-19-35(28(31(37)38)17-27(25)34)30(36)29(23-10-6-4-7-11-23)24-12-8-5-9-13-24/h4-16,20,28-29H,17-19H2,1-3H3,(H,37,38)
| Molecular Formula | C31H32N4O3 |
| Molecular Weight | 508.6108 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19038235
Curator's Comment: PD123319, administered peripherally, can cross the blood brain barrier to inhibit central AT2 receptors.
Originator
Sources: http://adisinsight.springer.com/drugs/800001732 | https://www.ncbi.nlm.nih.gov/pubmed/1956044
Curator's Comment: # Pfizer
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4607 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1956044 |
34.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Vasoactive role for angiotensin II type 2 receptors in human radial artery. | 2014-03-29 |
|
| Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. | 2005-09 |
|
| Increase in systemic blood pressure during intra-arterial PD123319 infusion: evidence for functional expression of angiotensin type 2 receptors in normal volunteers. | 2004 |
|
| Role of angiotensin type 2 receptors in human forearm vascular responses of normal volunteers. | 2001-09 |
|
| Induction of angiotensin II subtype 2 receptor-mediated blood pressure regulation in synthetic diet-fed rats. | 2000-09 |
|
| Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. | 1991-11 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16470490
Curator's Comment: Can also be used i.p. in rats (0.3mg/kg) https://www.ncbi.nlm.nih.gov/pubmed/25562714
and s.c in rats (1 mg/kg/day) https://www.ncbi.nlm.nih.gov/pubmed/19038235
Sixteen normal subjects received an intravenous infusion of PD123319 (10 mcg/minute for 5 minutes) and placebo, separated by one week.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24674681
The addition of 10(-6)M PD122319 to human arteries twenty minutes before
the stimulation of vasoconstriction by angiotensin
II caused a small but significant inhibition of
vasoconstriction by 20%. In other
arteries, the addition of 10(-6)M PD122319 twenty
minutes before the stimulation of vasoconstriction
by angiotensin II significantly enhanced
vasoconstriction, maximally by 60%.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Apr 02 21:02:43 GMT 2025
by
admin
on
Wed Apr 02 21:02:43 GMT 2025
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| Record UNII |
C2PJT3V6N6
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| Record Status |
Validated (UNII)
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| Record Version |
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114785-14-7
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| Related Record | Type | Details | ||
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ENANTIOMER -> RACEMATE |
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ENANTIOMER -> RACEMATE |
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