Uses
PD 123319 is a selective non-peptide angiotensin AT2 receptor antagonist.
Definition
ChEBI: An imidazopyridine consisting of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine having 4-(dimethylamino)-3-methylbenzyl, diphenylacetyl and carboxy and groups at positions 1, 5 and 6 respectively
Biological Activity
Potent, selective, non-peptide angiotensin AT 2 receptor antagonist. IC 50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.
Enzyme inhibitor
This potent non-peptide receptor antagonist (FW = 508.61 g/mol; CAS
130663-39-7), also named 1-[[4- (dimethylamino) -3-methylphenyl]methyl]-
5- (2,2-diphenylacetyl) -4,5,6,7-tetrahydro- (6S) -1H-imidazo[4,5-c]pyridine-
6-carboxylate, selectively targets AT2 angiotensin II receptor (IC50 = 34
nM). This class of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-
carboxylic acid derivatives displace 125I-labeled angiotensin II from a
specific subset of angiotensin II (Ang II) binding sites (that are different
from those mediating vascular contraction or aldosterone release) that are
likely to have novel properties. PD-123319 and another nonpeptide
antagonist (DuP-753) discriminate between two subclasses of All receptors
in many different tissues. PD 123319 does not influence baseline
cerebral blood flow, with minor drop in blood pressure.
References
[1] blankley c j, hodges j c, klutchko s r, et al. synthesis and structure-activity relationships of a novel series of non-peptide angiotensin ii receptor binding inhibitors specific for the at2 subtype. journal of medicinal chemistry, 1991, 34(11): 3248-3260.
[2] boulay g, servant g, luong t t, et al. modulation of angiotensin ii binding affinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of the dup-753-sensitive angiotensin ii receptor of bovine adrenal glomerulosa. molecular pharmacology, 1992, 41(4): 809-815.
[3] siragy h. angiotensin ii receptor blockers: review of the binding characteristics. the american journal of cardiology, 1999, 84(10): 3-8.