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dmp 811

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

DMP 811: angiotensin II receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	3081289
CHEMBL ID	115021
SCHEMBL ID	6556676
MeSH ID	M0227223

Synonyms (17)

Synonym
139964-19-5
4-ethyl-2-propyl-1-(2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methylimidazole-5-carboxylic acid
4-ethyl-2-propyl-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1h-imidazole-5-carboxylic acid
1h-imidazole-5-carboxylic acid, 4-ethyl-2-propyl-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
bdbm50049116
5-ethyl-2-propyl-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazole-4-carboxylic acid
5-ethyl-2-propyl-3-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazole-4-carboxylic acid
5-ethyl-2-propyl-3-(2''-tetrazol-1-yl-biphenyl-4-ylmethyl)-3h-imidazole-4-carboxylic acid
dmp 811
CHEMBL115021 ,
dmp-811
5-ethyl-2-propyl-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
4-ethyl-2-propyl-1-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]imidazole-5-carboxylic acid
OFYWYKMCRWMPPQ-UHFFFAOYSA-N ,
SCHEMBL6556676
dmp811
DTXSID40161205

Research Excerpts

Overview

DMP 811 is a diacidic angiotensin II antagonist.

Excerpt	Reference	Relevance
"DMP 811 is a diacidic angiotensin II antagonist. "	( Prodrugs to improve the oral bioavailability of a diacidic nonpeptide angiotensin II antagonist. Aungst, BJ; Blake, JA; Ensinger, CL; Hussain, MA; Pruitt, JR; Rogers, NJ; Saitoh, H, 1995)	1.73

Effects

Excerpt	Reference	Relevance
"DMP 811 has oral bioavailabilities of 7 and 29% in rats and dogs, respectively, after a solution dose and 8 and 13%, respectively, after a suspension or capsule dosing."	( Pharmacology and pharmacokinetics of a novel nonpeptide angiotensin II receptor antagonist--DMP 811. Agra, AM; Ardecky, RJ; Carini, DJ; Chiu, AT; Huang, SM; Price, WA; Timmermans, PB; Wexler, RR; Wong, PC, 1995)	1.23

Bioavailability

Excerpt	Reference	Relevance
" It has relatively low oral bioavailability in rats."	( Prodrugs to improve the oral bioavailability of a diacidic nonpeptide angiotensin II antagonist. Aungst, BJ; Blake, JA; Ensinger, CL; Hussain, MA; Pruitt, JR; Rogers, NJ; Saitoh, H, 1995)	0.29
" The oral bioavailability of DMP 811 was low, but consistent across species."	( Disposition of DMP 811 (L-708,404), a potent angiotensin II receptor antagonist, in the rat, monkey, and chimpanzee. Vyas, KP; Zhang, KE, 1995)	0.94

Dosage Studied

Excerpt	Relevance	Reference
" A simple n-propyl ester was hydrolyzed very slowly (< 10% in 24 hr) in rat plasma in vitro, and after oral dosing in rats plasma prodrug concentrations were much greater than DMP 811 concentrations."	( Prodrugs to improve the oral bioavailability of a diacidic nonpeptide angiotensin II antagonist. Aungst, BJ; Blake, JA; Ensinger, CL; Hussain, MA; Pruitt, JR; Rogers, NJ; Saitoh, H, 1995)	0.48

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Type-1A angiotensin II receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0060	0.0004	0.1555	3.8000	AID37837
Type-1B angiotensin II receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0060	0.0004	0.1334	3.8000	AID37837
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (11)

Assay ID	Title	Year	Journal	Article
AID18173	Oral bioavailability in dog	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID568790	Displacement of radiolabeled angiotensin2 from angiotensin AT1 receptor in rat adrenal cortex membranes	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID182953	In vivo inhibitory activity against angiotensin II induced pressor response in anesthetized normotensive rats	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID39641	In vitro for inhibition of [125I]-angiotensin II (0.1 nM) binding to angiotensin II receptor type 1 in membrane fractions of bovine adrenal cortex	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID568868	Antihypertensive activity in po dosed renal hypertensive rat model	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID37837	Inhibitory activity against Angiotensin II receptor type 1 in rat adrenal membrane	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID18175	Oral bioavailability in rat	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID568792	Antihypertensive activity in iv dosed renal hypertensive rat model	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID568880	Ratio of compound ED50 to losartan ED50 for po dosed renal hypertensive rat model	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID177204	Oral effective dose required for lowering blood pressure in renal hypertensive rats (RHR)	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID177200	Intravenous effective dose required for lowering blood pressure in renal hypertensive rats (RHR)	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	7 (77.78)	18.2507
2000's	1 (11.11)	29.6817
2010's	1 (11.11)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.90

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	11.90 (24.57)
Research Supply Index	2.30 (2.92)
Research Growth Index	4.20 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.90)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (22.22%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	7 (77.78%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
candesartan cilexetil candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects	4.03	2	biphenyls
candesartan candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.	4.03	2	benzimidazolecarboxylic acid; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.	4.03	2	azaspiro compound; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position	4.53	4	biphenylyltetrazole; imidazoles	angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist
dup 532 DuP 532: angiotensin I receptor antagonist	4.03	2
valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.	4.03	2	biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
tasosartan tasosartan: angiotensin II antagonist; structure given in first source	4.03	2	biphenyls
telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.	3.15	1	benzimidazoles; biphenyls; carboxybiphenyl	angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic
gr 117289 GR 117289: angiotensin AT1 receptor antagonist; structure given in first source. zolasartan : A member of the class of 1-benzofurans that is 3-bromo-1-benzofuran which is substituted by a 2-(1H-tetrazol-5-yl)phenyl group at position 2 and by a (2-butyl-5-carboxy-4-chloro-1H-imidazol-1-yl)methyl group at position 5. It is an angiotensin II receptor type 1 (AT1) antagonist and was in clinical trials for the treatment of hypertension (now discontinued).	4.03	2	1-benzofurans; biaryl; imidazolyl carboxylic acid; monocarboxylic acid; organobromine compound; organochlorine compound; tetrazoles	angiotensin receptor antagonist; antihypertensive agent
exp3174 losartan carboxylic acid: structure given in first source. losartan carboxylic acid : A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid.	4.31	3	biphenylyltetrazole; imidazoles; organochlorine compound	metabolite
exp7711 EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source	3.49	2
bibs 39 BIBS 39: structure given in first source; angiotensin II receptor antagonist	3.09	1
sc 51316 SC 51316: structure given in first source; an angiotensin II receptor antagonist	3.15	1
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3h-imidazo(4,5-b)pyridine 3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3H-imidazo(4,5-b)pyridine: a non-peptide angiotensin II-receptor antagonist; structure given in first source	4.03	2
a 81988 A 81988: angiotensin II antagonist selective for type 1 receptors	4.03	2
bibs 222 BIBS 222: structure given in first source; angiotensin II receptor antagonist	3.09	1
ici d8731 ICI D8731: structure given in first source; an angiotensin II receptor antagonist	4.03	2
forasartan forasartan: structure given in first source; an angiotensin AT(1) receptor antagonist; angiotensin II receptor antagonist; used in treatment of congestive heart failure. forasartan : A member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension.	4.03	2	benzenes; pyridines; tetrazoles; triazoles	angiotensin receptor antagonist; antihypertensive agent
up 269-6 UP 269-6: structure given in first source; angiotensin receptor antagonist	4.03	2
mk 996 MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source	4.03	2
olmesartan olmesartan: an active metabolite of CS 866	3.52	2	biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent
angiotensin ii Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).	7.91	4	amino acid zwitterion; angiotensin II	human metabolite
me 3221 ME 3221: an angiotensin II receptor antagonist; structure given in first source	4.03	2
l 158809 L 158809: RN & structure given in first source; angiotensin receptor antagonist	4.03	2
cv 11194 CV 11194: structure given in first source; an angiotensin II receptor antagonist	3.15	1
milfasartan milfasartan: angiotensin I receptor antagonist; structure in first source	4.03	2
eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.	4.03	2	dicarboxylic acid; imidazoles; thiophenes	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
exp 655 [no description available]	3.09	1
l 162313 L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95	3.09	1
pratosartan pratosartan: angiotensin II type 1 receptor blocker	4.03	2	biphenylyltetrazole	antihypertensive agent
l 163491 L 163491: structure given in first source	3.09	1
ema401 [no description available]	3.09	1
azilsartan azilsartan: an angiotensin type 1 receptor blocker; receptor blocker. azilsartan : A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) for treatment of hypertension.	3.15	1	1,2,4-oxadiazole; aromatic ether; benzimidazolecarboxylic acid	angiotensin receptor antagonist; antihypertensive agent

Condition	Relationship Strength	Studies
Cardiac Remodeling, Ventricular [description not available]	2	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	1.98	1
Goldblatt Syndrome [description not available]	1.98	1
Hypertension, Renovascular Hypertension due to RENAL ARTERY OBSTRUCTION or compression.	1.98	1

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