Perindopril

Identification

Summary

Perindopril is an ACE inhibitor prodrug used to treat hypertension, mild to moderate congestive heart failure, and to reduce cardiovascular risk in patients with hypertension or post-myocardial infarction.

Brand Names

Aceon, Coversyl, Prestalia, Viacoram

Generic Name

Perindopril

DrugBank Accession Number

DB00790

Background

Perindopril is a nonsulfhydryl prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly metabolized in the liver to perindoprilat, its active metabolite, following oral administration. Perindoprilat is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Perindopril may be used to treat mild to moderate essential hypertension, mild to moderate congestive heart failure, and to reduce the cardiovascular risk of individuals with hypertension or post-myocardial infarction and stable coronary disease.

Type

Small Molecule

Groups

Approved

Structure

Similar Structures

Weight: Average: 368.4678
Monoisotopic: 368.231122144
Chemical Formula: C₁₉H₃₂N₂O₅

Synonyms

(2S,3aS,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxopentan-2-yl]amino}propanoyl]octahydro-1H-indole-2-carboxylic acid
Perindopril
Perindoprilum

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Pharmacology

Indication

For the treatment of mild to moderate essential hypertension, mild to moderate congestive heart failure, and to reduce the cardiovascular risk of individuals with hypertension or post-myocardial infarction and stable coronary disease.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Used in combination to prevent	Cardiovascular events	Combination Product in combination with: Atorvastatin (DB01076)	••••••••••••	•••••	•••••••••• •••••••••• •• •••••••••••• •••••••••••••• •• ••••••••• •••••• •••• •••••••••••••• ••••	•••••••
Management of	Diabetic nephropathy		••• •••••
Management of	Essential hypertension		••••••••••••
Used in combination to manage	Hypertension	Combination Product in combination with: Amlodipine (DB00381)	••••••••••••		•••••••••• •••••••• •• ••••••••••• •••••••••••
Used in combination to manage	Hypertension	Combination Product in combination with: Indapamide (DB00808)	••••••••••••		•••••••••• •••••••• •• ••••••••••• •••••••••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Perindopril is a nonsulfhydryl prodrug that is metabolized via first pass effect (62%) and systemic hydrolysis (38%) to perindoprilat, its active metabolite, following oral administration. Perindoprilat lowers blood pressure by antagonizing the effect of the RAAS. The RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from the granular cells of the juxtaglomerular apparatus in the kidneys. In the blood stream, renin cleaves circulating angiotensinogen to ATI, which is subsequently cleaved to ATII by ACE. ATII increases blood pressure using a number of mechanisms. First, it stimulates the secretion of aldosterone from the adrenal cortex. Aldosterone travels to the distal convoluted tubule (DCT) and collecting tubule of nephrons where it increases sodium and water reabsorption by increasing the number of sodium channels and sodium-potassium ATPases on cell membranes. Second, ATII stimulates the secretion of vasopressin (also known as antidiuretic hormone or ADH) from the posterior pituitary gland. ADH stimulates further water reabsorption from the kidneys via insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules. Third, ATII increases blood pressure through direct arterial vasoconstriction. Stimulation of the Type 1 ATII receptor on vascular smooth muscle cells leads to a cascade of events resulting in myocyte contraction and vasoconstriction. In addition to these major effects, ATII induces the thirst response via stimulation of hypothalamic neurons. ACE inhibitors inhibit the rapid conversion of ATI to ATII and antagonize RAAS-induced increases in blood pressure. ACE (also known as kininase II) is also involved in the enzymatic deactivation of bradykinin, a vasodilator. Inhibiting the deactivation of bradykinin increases bradykinin levels and may sustain the effects of perindoprilat by causing increased vasodilation and decreased blood pressure.

Mechanism of action

There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Perindoprilat, the active metabolite of perindopril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Perindopril also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors.

Target	Actions	Organism
AAngiotensin-converting enzyme	inhibitor	Humans
USecreted frizzled-related protein 4	inhibitor	Humans

Absorption

Rapidly absorbed with peak plasma concentrations occurring approximately 1 hour after oral administration. Bioavailability is 65-75%. Following absorption, perindopril is hydrolyzed to perindoprilat, which has an average bioavailability of 20%. The rate and extent of absorption is unaffected by food. However, food decreases the extent of biotransformation to peridoprilat and reduces its bioavailability by 35%.

Volume of distribution

Not Available

Protein binding

Perindoprilat, 10-20% bound to plasma proteins

Metabolism

Extensively metabolized, with only 4-12% of the dose recovered in urine following oral administration. Six metabolites have been identified: perindoprilat, perindopril glucuronide, perindoprilat glucuronide, a perindopril lactam, and two perindoprilat lactams. Only perindoprilat is pharmacologically active. Peridoprilat and perindoprilat glucuronide are the two main circulating metabolites.

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Perindopril

Route of elimination

Perindopril is extensively metabolized following oral administration, with only 4 to 12% of the dose recovered unchanged in the urine.

Half-life

Perindopril, 1.2 hours; Peridoprilat, 30-120 hours. The long half life of peridoprilat is due to its slow dissociation from ACE binding sites.

Clearance

219 - 362 mL/min [oral administration]

Adverse Effects

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Toxicity

The most likely symptom of overdose is severe hypotension. The most common adverse effects observed in controlled clinical trials include cough, digestive symptoms, fatigue, headache, and dizziness.

Pathways

Pathway	Category
Perindopril Action Pathway	Drug action

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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Abacavir	Perindopril may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abaloparatide	The risk or severity of adverse effects can be increased when Perindopril is combined with Abaloparatide.
Acebutolol	Perindopril may increase the hypotensive activities of Acebutolol.
Aceclofenac	The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Perindopril.
Acemetacin	The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Acemetacin is combined with Perindopril.

Food Interactions

Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice).
Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
Limit salt intake. Salt may attenuate the antihypertensive effect.
Take with or without food. The absorption is unaffected by food.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Perindopril arginine	TFT5IM1KGB	612548-45-5	RYCSJJXKEWBUTI-YDYAIEMNSA-N
Perindopril erbumine	1964X464OJ	107133-36-8	IYNMDWMQHSMDDE-MHXJNQAMSA-N
Perindopril tosylate	G092350E9M	1258291-80-3	FWZROZSADJGJER-MHXJNQAMSA-N

Active Moieties

Name	Kind	UNII	CAS	InChI Key
Perindoprilat	prodrug	2UV6ZNQ92K	95153-31-4	ODAIHABQVKJNIY-PEDHHIEDSA-N

Product Images

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Aceon	Tablet	8 mg/1	Oral	Abbvie	2010-12-14	2014-01-01
Aceon	Tablet	8 mg/1	Oral	Symplmed Pharmaceuticals, Llc	2014-10-10	2017-03-01
Aceon	Tablet	4 mg/1	Oral	XOMA (US) LLC	1993-12-30	Not applicable
Aceon	Tablet	4 mg/1	Oral	Physicians Total Care, Inc.	2005-07-20	2011-06-30
Aceon	Tablet	4 mg/1	Oral	Abbvie	2010-12-14	2014-01-01

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Ag-perindopril	Tablet	8 mg	Oral	Angita Pharma Inc.	2018-12-24	Not applicable
Ag-perindopril	Tablet	4 mg	Oral	Angita Pharma Inc.	2018-12-24	Not applicable
Ag-perindopril	Tablet	2 mg	Oral	Angita Pharma Inc.	2018-12-24	Not applicable
Ag-perindopril Erbumine	Tablet	8 mg	Oral	Angita Pharma Inc.	2022-12-16	Not applicable
Ag-perindopril Erbumine	Tablet	4 mg	Oral	Angita Pharma Inc.	2022-12-16	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
ACEPER PLUS 2 MG/0.625 MG TABLET, 30 ADET	Perindopril erbumine (2 mg) + Indapamide (0.625 mg)	Tablet	Oral	GENVEON İLAÇ SAN. VE TİC. A.Ş.	2020-08-14	Not applicable
ACEPER PLUS 4 MG/1,25 MG TABLET, 30 ADET	Perindopril (4 mg) + Indapamide (1.25 mg)	Tablet	Oral	GENVEON İLAÇ SAN. VE TİC. A.Ş.	2011-05-05	Not applicable
AMLOPER 4/5MG FILM KAPLI TABLET, 30 ADET	Perindopril erbumine (4 mg) + Amlodipine besylate (5 mg)	Tablet, coated	Oral	CELTİS İLAÇ SAN. VE TİC. A.Ş.	2020-08-14	Not applicable
AMLOPER 4/5MG FILM KAPLI TABLET, 90 ADET	Perindopril erbumine (4 mg) + Amlodipine besylate (5 mg)	Tablet, coated	Oral	CELTİS İLAÇ SAN. VE TİC. A.Ş.	2013-03-26	Not applicable
AMLOPER 8/10MG FILM KAPLI TABLET, 30 ADET	Perindopril erbumine (8 mg) + Amlodipine besylate (10 mg)	Tablet, coated	Oral	CELTİS İLAÇ SAN. VE TİC. A.Ş.	2020-08-14	Not applicable

Chemical Identifiers

UNII: Y5GMK36KGY
CAS number: 82834-16-0
InChI Key: IPVQLZZIHOAWMC-QXKUPLGCSA-N
InChI: InChI=1S/C19H32N2O5/c1-4-8-14(19(25)26-5-2)20-12(3)17(22)21-15-10-7-6-9-13(15)11-16(21)18(23)24/h12-16,20H,4-11H2,1-3H3,(H,23,24)/t12-,13-,14-,15-,16-/m0/s1
IUPAC Name: (2S,3aS,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxopentan-2-yl]amino}propanoyl]-octahydro-1H-indole-2-carboxylic acid
SMILES: [H][C@]12C[C@H](N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@@]1([H])CCCC2)C(O)=O

References

Synthesis Reference

Michel Vincent, Jean Baliarda, Bernard Marchand, Georges Remond, "Process for the industrial synthesis of perindopril." U.S. Patent US4914214, issued April 03, 1990.

US4914214

General References

Hurst M, Jarvis B: Perindopril: an updated review of its use in hypertension. Drugs. 2001;61(6):867-96. [Article]
Jastrzebskal M, Widecka K, Naruszewicz M, Ciechanowicz A, Janczak-Bazan A, Foltynska A, Goracy I, Chetstowski K, Wesotowska T: Effects of perindopril treatment on hemostatic function in patients with essential hypertension in relation to angiotensin converting enzyme (ACE) and plasminogen activator inhibitor-1 (PAI-1) gene polymorphisms. Nutr Metab Cardiovasc Dis. 2004 Oct;14(5):259-69. [Article]
Parker E, Aarons L, Rowland M, Resplandy G: The pharmacokinetics of perindoprilat in normal volunteers and patients: influence of age and disease state. Eur J Pharm Sci. 2005 Sep;26(1):104-13. [Article]
Simpson D, Noble S, Goa KL: Perindopril: in congestive heart failure. Drugs. 2002;62(9):1367-77; discussion 1378-9. [Article]
Yasumatsu R, Nakashima T, Masuda M, Ito A, Kuratomi Y, Nakagawa T, Komune S: Effects of the angiotensin-I converting enzyme inhibitor perindopril on tumor growth and angiogenesis in head and neck squamous cell carcinoma cells. J Cancer Res Clin Oncol. 2004 Oct;130(10):567-73. Epub 2004 Jul 27. [Article]
Yoshiji H, Kuriyama S, Kawata M, Yoshii J, Ikenaka Y, Noguchi R, Nakatani T, Tsujinoue H, Fukui H: The angiotensin-I-converting enzyme inhibitor perindopril suppresses tumor growth and angiogenesis: possible role of the vascular endothelial growth factor. Clin Cancer Res. 2001 Apr;7(4):1073-8. [Article]

External Links

Human Metabolome Database: HMDB0014928
KEGG Drug: D03753
KEGG Compound: C07706
PubChem Compound: 107807
PubChem Substance: 46508767
ChemSpider: 96956
BindingDB: 50493988
RxNav: 54552
ChEBI: 8024
ChEMBL: CHEMBL1581
ZINC: ZINC000003812867
Therapeutic Targets Database: DNC001114
PharmGKB: PA450877
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
PDRhealth: PDRhealth Drug Page
Wikipedia: Perindopril

FDA label

Download (149 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Blood Pressures / Chronic Kidney Disease (CKD) / Proteinuria	1
4	Completed	Treatment	Hypertension	6
4	Completed	Treatment	Hypertension / Hyperuricemia / Menopause	1
4	Completed	Treatment	Hypertension / Type 2 Diabetes Mellitus	2
4	Completed	Treatment	Induction of Intraoperative Hypotension	1

Pharmacoeconomics

Manufacturers

Abbott products inc
Aurobindo pharma ltd
Ivax pharmaceuticals inc
Lupin ltd
Roxane laboratories inc

Packagers

Aurobindo Pharma Ltd.
Inyx Usa Ltd.
Ipca Laboratories Ltd.
Lupin Pharmaceuticals Inc.
Murfreesboro Pharmaceutical Nursing Supply
Roxane Labs
Servier Canada Inc.
Solvay Pharmaceuticals

Dosage Forms

Form	Route	Strength
Tablet, coated	Oral
Tablet	Oral	10 mg
Tablet	Oral	2.5 mg
Tablet	Oral	5 mg
Tablet, film coated	Oral
Tablet, film coated	Oral	2.5 MG
Tablet	Oral	2 mg
Tablet, film coated	Oral	6.790 mg
Tablet	Oral	4 mg
Tablet, film coated	Oral	3.395 mg
Tablet, coated	Oral	10 mg
Tablet, coated	Oral	5 mg
Tablet, orally disintegrating	Oral	10 mg
Tablet, orally disintegrating	Oral	2.5 mg
Tablet, orally disintegrating	Oral	5 mg
Tablet, film coated	Oral	0.625 mg
Tablet, film coated	Oral	1.25 mg
Tablet	Oral	1.25 mg
Tablet	Oral	8 mg
Capsule	Oral
Tablet	Oral	4.00 mg
Tablet	Oral
Tablet, film coated, extended release	Oral
Tablet, film coated	Oral	2 mg
Tablet, film coated	Oral	4 mg
Tablet	Oral	2 mg/1
Tablet	Oral	4 mg/1
Tablet	Oral	8 mg/1
Tablet	Oral	4.0 mg
Tablet, coated	Oral	2.5 mg
Tablet	Oral
Tablet	Oral	0.625 mg
Tablet, film coated	Oral
Tablet, film coated	Oral	5 mg
Tablet, film coated	Oral	10 mg
Tablet, film coated	Oral	10 mg
Tablet, film coated	Oral	5 mg

Prices

Unit description	Cost	Unit
Aceon 8 mg tablet	3.14USD	tablet
Perindopril erbumine 8 mg tablet	2.8USD	tablet
Aceon 4 mg tablet	2.58USD	tablet
Perindopril erbumine 4 mg tablet	2.3USD	tablet
Aceon 2 mg tablet	2.22USD	tablet
Perindopril erbumine 2 mg tablet	1.98USD	tablet
Coversyl 8 mg Tablet	1.23USD	tablet
Coversyl 4 mg Tablet	0.88USD	tablet
Coversyl 2 mg Tablet	0.7USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US5162362	No	1992-11-10	2009-11-10
CA2473205	No	2010-05-18	2023-01-22
CA1341196	No	2001-03-06	2018-03-06
US7846961	No	2010-12-07	2029-10-05
US6696481	No	2004-02-24	2023-04-15

Properties

State

Solid

Experimental Properties

Property	Value	Source
logP	2.6	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	1.22 mg/mL	ALOGPS
logP	0.56	ALOGPS
logP	0.63	Chemaxon
logS	-2.5	ALOGPS
pKa (Strongest Acidic)	3.79	Chemaxon
pKa (Strongest Basic)	5.48	Chemaxon
Physiological Charge	-1	Chemaxon
Hydrogen Acceptor Count	5	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	95.94 Å²	Chemaxon
Rotatable Bond Count	9	Chemaxon
Refractivity	95.69 m³·mol^-1	Chemaxon
Polarizability	39.99 Å³	Chemaxon
Number of Rings	2	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9156
Blood Brain Barrier	-	0.8411
Caco-2 permeable	-	0.7871
P-glycoprotein substrate	Substrate	0.6826
P-glycoprotein inhibitor I	Inhibitor	0.5
P-glycoprotein inhibitor II	Inhibitor	0.8589
Renal organic cation transporter	Non-inhibitor	0.919
CYP450 2C9 substrate	Non-substrate	0.8638
CYP450 2D6 substrate	Non-substrate	0.8542
CYP450 3A4 substrate	Substrate	0.549
CYP450 1A2 substrate	Non-inhibitor	0.8796
CYP450 2C9 inhibitor	Non-inhibitor	0.8612
CYP450 2D6 inhibitor	Non-inhibitor	0.9088
CYP450 2C19 inhibitor	Non-inhibitor	0.8375
CYP450 3A4 inhibitor	Non-inhibitor	0.7142
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.5951
Ames test	Non AMES toxic	0.8814
Carcinogenicity	Non-carcinogens	0.9266
Biodegradation	Not ready biodegradable	0.9082
Rat acute toxicity	1.9432 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9839
hERG inhibition (predictor II)	Non-inhibitor	0.8678

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-006t-9432000000-cd5a3e77250a4c168d5f
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-014j-1039000000-b957a673d9629f4c21ea
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-014r-0009000000-334d0b178dc9f6fc18de
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0005-8964000000-9f0d93ae0e844e61b5b0
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0gb9-2913000000-f04e410ea5b599a6f73b
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-014i-0900000000-602da46b0a9be040723d
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-00dj-5920000000-78c3bf8e9c381d8424f8
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	202.7032343	predicted	DarkChem Lite v0.1.0
[M-H]-	195.1227	predicted	DeepCCS 1.0 (2019)
[M+H]+	203.5029343	predicted	DarkChem Lite v0.1.0
[M+H]+	197.51825	predicted	DeepCCS 1.0 (2019)
[M+Na]+	202.3678343	predicted	DarkChem Lite v0.1.0
[M+Na]+	203.4308	predicted	DeepCCS 1.0 (2019)

Targets

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Details1. Angiotensin-converting enzyme

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Zinc ion binding
Specific Function: Converts angiotensin I to angiotensin II by release of the terminal His-Leu, this results in an increase of the vasoconstrictor activity of angiotensin. Also able to inactivate bradykinin, a potent...
Gene Name: ACE
Uniprot ID: P12821
Uniprot Name: Angiotensin-converting enzyme
Molecular Weight: 149713.675 Da

References

Alfakih K, Hall AS: Perindopril. Expert Opin Pharmacother. 2006 Jan;7(1):63-71. [Article]
Brugts JJ, Ferrari R, Simoons ML: Angiotensin-converting enzyme inhibition by perindopril in the treatment of cardiovascular disease. Expert Rev Cardiovasc Ther. 2009 Apr;7(4):345-60. doi: 10.1586/erc.09.2. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Song JC, White CM: Clinical pharmacokinetics and selective pharmacodynamics of new angiotensin converting enzyme inhibitors: an update. Clin Pharmacokinet. 2002;41(3):207-24. [Article]

Details2. Secreted frizzled-related protein 4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Soluble frizzled-related proteins (sFRPS) function as modulators of Wnt signaling through direct interaction with Wnts. They have a role in regulating cell growth and differentiation in specific cell types (By similarity). SFRP4 plays a role in bone morphogenesis. May also act as a regulator of adult uterine morphology and function. May also increase apoptosis during ovulation possibly through modulation of FZ1/FZ4/WNT4 signaling (By similarity). Has phosphaturic effects by specifically inhibiting sodium-dependent phosphate uptake (PubMed:12952927).
Specific Function: Wnt-protein binding
Gene Name: SFRP4
Uniprot ID: Q6FHJ7
Uniprot Name: Secreted frizzled-related protein 4
Molecular Weight: 39826.305 Da

References

Bukhari SA, Shamshari WA, Ur-Rahman M, Zia-Ul-Haq M, Jaafar HZ: Computer aided screening of secreted frizzled-related protein 4 (SFRP4): a potential control for diabetes mellitus. Molecules. 2014 Jul 11;19(7):10129-36. doi: 10.3390/molecules190710129. [Article]

Enzymes

Details1. Cholinesterase

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Identical protein binding
Specific Function: Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name: BCHE
Uniprot ID: P06276
Uniprot Name: Cholinesterase
Molecular Weight: 68417.575 Da

References

Mehta A, Iyer L, Parmar S, Shah G, Goyal R: Oculohypotensive effect of perindopril in acute and chronic models of glaucoma in rabbits. Can J Physiol Pharmacol. 2010 May;88(5):595-600. doi: 10.1139/y10-026. [Article]

Transporters

Details1. Solute carrier family 15 member 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Proton-dependent oligopeptide secondary active transmembrane transporter activity
Specific Function: Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
Gene Name: SLC15A1
Uniprot ID: P46059
Uniprot Name: Solute carrier family 15 member 1
Molecular Weight: 78805.265 Da

References

Knutter I, Wollesky C, Kottra G, Hahn MG, Fischer W, Zebisch K, Neubert RH, Daniel H, Brandsch M: Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited. J Pharmacol Exp Ther. 2008 Nov;327(2):432-41. doi: 10.1124/jpet.108.143339. Epub 2008 Aug 19. [Article]

Details2. Solute carrier family 15 member 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Peptide:proton symporter activity
Specific Function: Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides.
Gene Name: SLC15A2
Uniprot ID: Q16348
Uniprot Name: Solute carrier family 15 member 2
Molecular Weight: 81782.77 Da

References

Knutter I, Wollesky C, Kottra G, Hahn MG, Fischer W, Zebisch K, Neubert RH, Daniel H, Brandsch M: Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited. J Pharmacol Exp Ther. 2008 Nov;327(2):432-41. doi: 10.1124/jpet.108.143339. Epub 2008 Aug 19. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55

Perindopril

Identification

Structure for Perindopril (DB00790)

Pharmacology

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Pharmacoeconomics

Properties

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Enzymes

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Transporters

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