Target Information

Target General Information

Target ID

T74456 (Former ID: TTDS00267)

Target Name

Angiotensin II receptor type-1 (AGTR1)

Synonyms

Type-1 angiotensin II receptor; Angiotensin II type-1 receptor; Angiotensin II receptor 1; Angiotensin 1 receptor; AT2R1B; AT2R1; AT1BR; AT1AR; AT1; AGTR1B; AGTR1A

Gene Name

AGTR1

Target Type

Successful target

[1]

Disease

[+] 3 Target-related Diseases

Essential hypertension [ICD-11: BA00]

Hypertension [ICD-11: BA00-BA04]

Secondary hypertension [ICD-11: BA04]

Function

Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Receptor for angiotensin II.

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BioChemical Class

GPCR rhodopsin

UniProt ID

AGTR1_HUMAN

Sequence

MILNSSTEDGIKRIQDDCPKAGRHNYIFVMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLK
TVASVFLLNLALADLCFLLTLPLWAVYTAMEYRWPFGNYLCKIASASVSFNLYASVFLLT
CLSIDRYLAIVHPMKSRLRRTMLVAKVTCIIIWLLAGLASLPAIIHRNVFFIENTNITVC
AFHYESQNSTLPIGLGLTKNILGFLFPFLIILTSYTLIWKALKKAYEIQKNKPRNDDIFK
IIMAIVLFFFFSWIPHQIFTFLDVLIQLGIIRDCRIADIVDTAMPITICIAYFNNCLNPL
FYGFLGKKFKRYFLQLLKYIPPKAKSHSNLSTKMSTLSYRPSDNVSSSTKKPAPCFEVE

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

HIT2.0 ID

T23RWU

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 15 Approved Drugs

ANGIOTENSIN II

Drug Info

Approved

Increase blood pressure

[2]

Azilsartan

Drug Info

Approved

Hypertension

[3], [4]

Candesartan

Drug Info

Approved

Hypertension

[5], [6]

Eprosartan

Drug Info

Approved

Hypertension

[6], [7]

Forasartan

Drug Info

Approved

Hypertension

[8], [9]

Irbesartan

Drug Info

Approved

Hypertension

[10], [11]

Losartan

Drug Info

Approved

Hypertension

[11], [12]

Micardis telmisartan

Drug Info

Approved

Hypertension

[13]

Olmesartan medoxomil

Drug Info

Approved

High blood pressure

[14]

Saprisartan

Drug Info

Approved

Hypertension

[15], [16]

SARALASIN

Drug Info

Approved

Hypertension

[17], [18]

Saralasin Acetate

Drug Info

Approved

Hypertension

[18]

Tasosartan

Drug Info

Approved

Hypertension

[6], [19]

Telmisartan

Drug Info

Approved

Hypertension

[6], [20]

Valsartan

Drug Info

Approved

Hypertension

[6], [21]

Clinical Trial Drug(s)

[+] 7 Clinical Trial Drugs

Pratosartan

Drug Info

Phase 3

Hypertension

[22]

S-474474

Drug Info

Phase 3

Metabolic syndrome x

[23]

sparsentan

Drug Info

Phase 3

Focal segmental glomerulosclerosis

[24]

TAK-491

Drug Info

Phase 3

Hypertension

[25]

CL-329167

Drug Info

Phase 2

Hypertension

[26]

TRV027

Drug Info

Phase 2

Heart failure

[27]

YM-358

Drug Info

Phase 2

Hypertension

[28]

Discontinued Drug(s)

[+] 13 Discontinued Drugs

KRH-594

Drug Info

Discontinued in Phase 2

Hypertension

[29]

MILFASARTAN

Drug Info

Discontinued in Phase 2

Hypertension

[30]

RIPISARTAN

Drug Info

Discontinued in Phase 2

Hypertension

[31]

Zolasartan

Drug Info

Discontinued in Phase 2

Hypotension

[32]

TAK-591

Drug Info

Discontinued in Phase 1

Hypertension

[33]

UR-7198

Drug Info

Discontinued in Phase 1

Hypertension

[34]

A-81988

Drug Info

Terminated

Hypertension

[35]

CR-3834

Drug Info

Terminated

Hypertension

[36]

L-158809

Drug Info

Terminated

Hypertension

[37]

L-159689

Drug Info

Terminated

Hypertension

[38]

RS-66252

Drug Info

Terminated

Alzheimer disease

[39]

UP-275-22

Drug Info

Terminated

Hypertension

[40]

XR-510

Drug Info

Terminated

Hypertension

[41]

Mode of Action

[+] 5 Modes of Action

Inhibitor

[+] 20 Inhibitor drugs

ANGIOTENSIN II

Drug Info

[42]

SARALASIN

Drug Info

[56]

HELENALIN

Drug Info

[74]

L-159689

Drug Info

[62]

4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol

Drug Info

[80]

CV-11194

Drug Info

[86]

GNF-PF-2307

Drug Info

[74]

GNF-PF-2812

Drug Info

[74]

GNF-PF-3832

Drug Info

[74]

L-159093

Drug Info

[62]

L-162313

Drug Info

[89]

L-162782

Drug Info

[89]

[Bpa1]AngII

Drug Info

[42]

[Sar1,Bpa2]AngII

Drug Info

[42]

[Sar1,Bpa3]AngII

Drug Info

[42]

[Sar1,Bpa8]AngII

Drug Info

[42]

[Sar1,Tdf2]AngII

Drug Info

[42]

[Sar1,Tdf3]AngII

Drug Info

[42]

[Sar1,Tdf8]AngII

Drug Info

[42]

[Tdf1]AngII

Drug Info

[42]

Modulator

[+] 7 Modulator drugs

Azilsartan

Drug Info

[43]

Saralasin Acetate

Drug Info

[57]

TAK-491

Drug Info

[43]

RS-66252

Drug Info

[76]

UP-275-22

Drug Info

[77]

XR-510

Drug Info

[78]

CGP-49870

Drug Info

[85]

Antagonist

[+] 35 Antagonist drugs

Candesartan

Drug Info

[44], [45], [46]

Eprosartan

Drug Info

[47], [48]

Forasartan

Drug Info

[9], [49]

Irbesartan

Drug Info

[1], [50]

Losartan

Drug Info

[1], [51], [52], [53]

Micardis telmisartan

Drug Info

[54]

Olmesartan medoxomil

Drug Info

[55]

Saprisartan

Drug Info

[16]

Tasosartan

Drug Info

[58]

Telmisartan

Drug Info

[59]

Valsartan

Drug Info

[1], [51], [60]

Pratosartan

Drug Info

[61]

sparsentan

Drug Info

[62]

CL-329167

Drug Info

[63], [18]

TRV027

Drug Info

[64]

YM-358

Drug Info

[65], [18]

KRH-594

Drug Info

[66]

MILFASARTAN

Drug Info

[67], [18]

RIPISARTAN

Drug Info

[68], [18]

TAK-591

Drug Info

[70]

UR-7198

Drug Info

[71]

A-81988

Drug Info

[72]

CR-3834

Drug Info

[73]

L-158809

Drug Info

[75]

(E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n

Drug Info

[79]

4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone

Drug Info

[81]

4-[(diphenylmethyl)amino]-2-phenylquinazoline

Drug Info

[82]

5-butyl-methyl immidazole carboxylate 30

Drug Info

[83]

5-oxo-1-2-4-oxadiazol biphenyl

Drug Info

[84]

EXP3174

Drug Info

[87], [88]

LY301875

Drug Info

[91]

LY303336

Drug Info

[91]

N,N`-bis-alkyl butylimmidazole 12b

Drug Info

[92]

[125I]EXP985

Drug Info

[93]

[3H]GBR12935

Drug Info

[94]

Blocker

[+] 1 Blocker drugs

S-474474

Drug Info

[23]

Agonist

[+] 3 Agonist drugs

Zolasartan

Drug Info

[69]

angiotensin III

Drug Info

[77]

L-163,101

Drug Info

[90]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

Top

Target-regulating microRNAs

Target-regulating microRNAs Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 8 KEGG Pathways

Calcium signaling pathway

cGMP-PKG signaling pathway

Neuroactive ligand-receptor interaction

Adrenergic signaling in cardiomyocytes

Vascular smooth muscle contraction

Renin-angiotensin system

Renin secretion

Pathways in cancer

NetPath Pathway

[+] 1 NetPath Pathways

TGF_beta_Receptor Signaling Pathway

Panther Pathway

[+] 1 Panther Pathways

Angiotensin II-stimulated signaling through G proteins and beta-arrestin

Pathwhiz Pathway

[+] 2 Pathwhiz Pathways

Angiotensin Metabolism

Muscle/Heart Contraction

PID Pathway

[+] 3 PID Pathways

Arf6 trafficking events

Arf6 signaling events

Angiopoietin receptor Tie2-mediated signaling

Reactome

[+] 2 Reactome Pathways

Peptide ligand-binding receptors

G alpha (q) signalling events

WikiPathways

[+] 7 WikiPathways

ACE Inhibitor Pathway

GPCRs, Class A Rhodopsin-like

Gastrin-CREB signalling pathway via PKC and MAPK

Peptide GPCRs

Allograft Rejection

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

Target QSAR Model

References

Top

REF 1

Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.

REF 2

2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.

REF 3

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6901).

REF 4

Clinical pipeline report, company report or official report of Takeda.

REF 5

REF 6

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 7

REF 8

REF 9

Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification. J Med Chem. 2003 Feb 27;46(5):716-26.

REF 10

REF 11

New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.

REF 12

REF 13

Clinical pipeline report, company report or official report of Boehringer-Ingelheim Pharmaceuticals.

REF 14

Effect of angiotensin receptor blockade on endothelial function: focus on olmesartan medoxomil. Vasc Health Risk Manag. 2009;5(1):301-14.

REF 15

REF 16

Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol. 1999 Nov;15 Suppl F:26F-8F.

REF 17

REF 18

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 19

REF 20

REF 21

REF 22

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002623)

REF 23

Clinical pipeline report, company report or official report of Shionogi (2011).

REF 24

ClinicalTrials.gov (NCT03493685) Study of Sparsentan in Patients With Primary Focal Segmental Glomerulosclerosis (FSGS) (DUPLEX). U.S. National Institutes of Health.

REF 25

ClinicalTrials.gov (NCT02480764) TAK-491 (Azilsartan Medoxomil) Compared to Valsartan in Chinese Participants With Hypertension.

REF 26

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004990)

REF 27

ClinicalTrials.gov (NCT01966601) A Study to Explore the Efficacy of TRV027 in Patients Hospitalized for Acute Decompensated Heart Failure. U.S. National Institutes of Health.

REF 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002583)

REF 29

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007913)

REF 30

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002993)

REF 31

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004530)

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001788)

REF 33

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028308)

REF 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010597)

REF 35

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002509)

REF 36

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022642)

REF 37

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001562)

REF 38

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003495)

REF 39

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007561)

REF 40

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004864)

REF 41

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004861)

REF 42

The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1. J Med Chem. 2010 Mar 11;53(5):2063-75.

REF 43

2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.

REF 44

Candesartan: widening indications for this angiotensin II receptor blocker Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007.

REF 45

Angiotensin II type 1 receptor blockade: a novel therapeutic concept. Blood Press Suppl. 2000;1:9-13.

REF 46

Binding of the antagonist [3H]candesartan to angiotensin II AT1 receptor-transfected [correction of tranfected] Chinese hamster ovary cells. Eur J Pharmacol. 1999 Feb 19;367(2-3):413-22.

REF 47

Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7.

REF 48

Characterization of [3H]SK&F 108566 as a radioligand for angiotensin type-1 receptor. J Recept Res. 1993;13(5):849-61.

REF 49

Possible involvement of calcium-calmodulin pathways in the positive chronotropic response to angiotensin II on the canine cardiac sympathetic ganglia. Jpn J Pharmacol. 2001 Aug;86(4):381-9.

REF 50

Binding characteristics of [(3)H]-irbesartan to human recombinant angiotensin type 1 receptors. J Renin Angiotensin Aldosterone Syst. 2000 Jun;1(2):159-65.

REF 51

Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.

REF 52

Effect of episodic hypoxia on sympathetic activity and blood pressure. Respir Physiol. 2000 Feb;119(2-3):189-97.

REF 53

Characterization of [3H]losartan receptors in isolated rat glomeruli. Eur J Pharmacol. 1993 Oct 15;247(2):193-8.

REF 54

The angiotensin II receptor antagonist telmisartan reduces urinary albumin excretion in patients with isolated systolic hypertension: results of a randomized, double-blind, placebo-controlled trial. J Hypertens. 2005 Nov;23(11):2055-61.

REF 55

Mechanism of diastolic stiffening of the failing myocardium and its prevention by angiotensin receptor and calcium channel blockers. J Cardiovasc Pharmacol. 2009 Jul;54(1):47-56.

REF 56

Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.

REF 57

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 58

Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54.

REF 59

Deletion of angiotensin II type I receptor reduces hepatic steatosis. J Hepatol. 2009 Jun;50(6):1226-35.

REF 60

Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors. Fundam Clin Pharmacol. 2000 Nov-Dec;14(6):577-85.

REF 61

Clinical efficacy of a new angiotensin II type 1 receptor blocker, pratosartan, in hypertensive patients. Hypertens Res. 2008 Feb;31(2):281-7.

REF 62

Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.

REF 63

Distribution and function of cardiac angiotensin AT1- and AT2-receptor subtypes in hypertrophied rat hearts. Am J Physiol. 1994 Aug;267(2 Pt 2):H844-52.

REF 64

First clinical experience with TRV027: pharmacokinetics and pharmacodynamics in healthy volunteers. J Clin Pharmacol. 2013 Sep;53(9):892-9.

REF 65

Effects of YM358, an angiotensin II type 1 (AT1) receptor antagonist, and enalapril on blood pressure and vasoconstriction in two renal hypertension models. Biol Pharm Bull. 2000 Feb;23(2):174-81.

REF 66

Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors. Fundam Clin Pharmacol. 2002 Aug;16(4):317-23.

REF 67

Dual action molecules: bioassays of combined novel antioxidants and angiotensin II receptor antagonists. Eur J Pharmacol. 2012 Nov 15;695(1-3):96-103.

REF 68

In vitro pharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist. Fundam Clin Pharmacol. 1995;9(2):119-28.

REF 69

Azilsartan: a newly approved angiotensin II receptor blocker. Cardiol Rev. 2011 Nov-Dec;19(6):300-4.

REF 70

Clinical pipeline report, company report or official report of Takeda (2009).

REF 71

Pharmacologic profile of UR-7247, an orally active angiotensin II AT1 receptor antagonist, in healthy volunteers. p6. J Cardiovasc Pharmacol. 2000 Mar;35(3):383-9.

REF 72

[3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors. Eur J Pharmacol. 1994 Mar 15;267(1):49-54.

REF 73

Pharmacokinetic study of a new angiotensin-AT1 antagonist by HPLC. J Pharm Biomed Anal. 2008 Sep 29;48(2):422-7.

REF 74

In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.

REF 75

Characterization of the binding of [3H]L-158,809: a new potent and selective nonpeptide angiotensin II receptor (AT1) antagonist radioligand. Mol Pharmacol. 1992 Dec;42(6):1077-82.

REF 76

Virtual Screening in Drug Discovery, Juan Alvarez Brian Shoichet. Page(218).

REF 77

REF 78

Pharmacology of XR510, a potent orally active nonpeptide angiotensin II AT1 receptor antagonist with high affinity for the AT2 receptor subtype. J Cardiovasc Pharmacol. 1995 Sep;26(3):354-62.

REF 79

Pharmacological characterization of (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n ortropane as a selective and potent inhibitor of the neuronal dopamine transporter. J Pharmacol Exp Ther. 1999 Nov;291(2):648-54.

REF 80

Discovery and development of aryl-fused imidazole-based angiotensin II antagonists, Bioorg. Med. Chem. Lett. 4(1):213-218 (1994).

REF 81

Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies. J Med Chem. 2000 Feb 10;43(3):351-60.

REF 82

Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2225-8.

REF 83

The discovery of new potent non-peptide Angiotensin II AT1 receptor blockers: a concise synthesis, molecular docking studies and biological evaluation of N-substituted 5-butylimidazole derivatives. Eur J Med Chem. 2012 Sep;55:358-74.

REF 84

Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect. Bioorg Med Chem. 2012 Apr 15;20(8):2747-61.

REF 85

Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and AT1 receptor antagonists

REF 86

Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisoste... J Med Chem. 1996 Dec 20;39(26):5228-35.

REF 87

Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol Rev. 1993 Jun;45(2):205-51.

REF 88

Angiotensin II receptor antagonists: imidazoles and pyrroles bearing hydroxymethyl and carboxy substituents, Bioorg. Med. Chem. Lett. 4(1):177-182 (1994).

REF 89

Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships. Bioorg Med Chem. 2008 Jul 15;16(14):6841-9.

REF 90

Structural model of antagonist and agonist binding to the angiotensin II, AT1 subtype, G protein coupled receptor. Chem Biol. 1994 Dec;1(4):211-21.

REF 91

Inhibition of angiotensin II-induced inositol phosphate production by triacid nonpeptide antagonists in CHO cells expressing human AT1 receptors. Pharm Res. 2000 Dec;17(12):1482-8.

REF 92

Rational design, efficient syntheses and biological evaluation of N,N'-symmetrically bis-substituted butylimidazole analogs as a new class of potent Angiotensin II receptor blockers. Eur J Med Chem. 2013 Apr;62:352-70.

REF 93

[125I]EXP985: a highly potent and specific nonpeptide radioligand antagonist for the AT1 angiotensin receptor. Biochem Biophys Res Commun. 1992 Nov 16;188(3):1030-9.

REF 94

Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem Pharmacol. 1997 Jun 15;53(12):1937-9.

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