Identification

Name
Brompheniramine
Accession Number
DB00835  (APRD00832)
Type
Small Molecule
Groups
Approved
Description

Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria. [PubChem]

Structure
Thumb
Synonyms
  • [3-(4-Bromo-phenyl)-3-pyridin-2-yl-propyl]-dimethyl-amine
  • 1-(P-Bromophenyl)-1-(2-pyridyl)-3-dimethylaminopropane
  • 2-(P-Bromo-alpha-(2-dimethylaminoethyl)benzyl)pyridine
  • 3-(4-Bromophenyl)-N,N-dimethyl-3-(2-pyridinyl)-1-propanamine
  • 3-(P-Bromophenyl)-3-(2-pyridyl)-N,N-dimethylpropylamine
  • BPN
  • Bromfeniramina
  • Brompheniramin
  • Bromphéniramine
  • Brompheniraminum
External IDs
AHR 1843 / D 721
Product Ingredients
IngredientUNIICASInChI Key
Brompheniramine maleateIXA7C9ZN03980-71-2SRGKFVAASLQVBO-BTJKTKAUSA-N
Product Images
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dimegan Inj 10mg/mlLiquid10 mgIntramuscular; SubcutaneousDexo Sa Labs Pharms1988-12-311997-05-30Canada
Dimetane Elixir 2mg/5mlElixir2 mgOralWhitehall Robins Inc.1993-12-311997-08-07Canada
Dimetane Tab 4mgTablet4 mgOralWhitehall Robins Inc.1957-12-312000-07-26Canada
J-tan PdLiquid1 mg/1mLOralJaymac Pharmaceuticals Llc2007-05-292016-08-01Us
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
7 Select Cold and Allergy ChildrensBrompheniramine maleate (1 mg/5mL) + Phenylephrine hydrochloride (2.5 mg/5mL)LiquidOral7 Eleven2014-08-052016-02-19Us
Alahist DMBrompheniramine maleate (4 mg/5mL) + Dextromethorphan hydrobromide monohydrate (15 mg/5mL) + Phenylephrine hydrochloride (7.5 mg/5mL)LiquidOralPoly Pharmaceuticals2007-12-272018-02-01Us
Altidec ABrompheniramine maleate (2 mg/5mL) + Phenylephrine hydrochloride (5 mg/5mL)LiquidOralAlternative Pharmacal Corporation2015-03-012017-01-01Us
Altipres-BBrompheniramine maleate (4 mg/5mL) + Dextromethorphan hydrobromide monohydrate (20 mg/5mL) + Phenylephrine hydrochloride (10 mg/5mL)LiquidOralAlternative Pharmacal Corporation2012-11-01Not applicableUs
AP-Hist DMBrompheniramine maleate (4 mg/1mL) + Dextromethorphan hydrobromide monohydrate (15 mg/1mL) + Phenylephrine hydrochloride (7.5 mg/1mL)LiquidOralAllegis Pharmaceuticals, LLC2013-04-15Not applicableUs
Assured Childrens Cold and CoughBrompheniramine maleate (1 mg/5mL) + Dextromethorphan hydrobromide monohydrate (5 mg/5mL) + Phenylephrine hydrochloride (2.5 mg/5mL)LiquidOralBio Pharm, Inc.2011-11-012018-08-27Us
Atuss DaBrompheniramine maleate (2 mg/5mL) + Chlophedianol hydrochloride (12.5 mg/5mL) + Pseudoephedrine hydrochloride (30 mg/5mL)LiquidOralCarwin Associates, Inc2016-10-25Not applicableUs
Atuss DaBrompheniramine maleate (2 mg/5mL) + Chlophedianol hydrochloride (12.5 mg/5mL) + Pseudoephedrine hydrochloride (30 mg/5mL)LiquidOralMagna Pharmceuticals, Inc.2018-11-20Not applicableUs
Atuss DaBrompheniramine maleate (2 mg/5mL) + Chlophedianol hydrochloride (12.5 mg/5mL) + Pseudoephedrine hydrochloride (30 mg/5mL)LiquidOralAber Pharmaceuticals, Llc2016-02-08Not applicableUs
Auro Tap Childrens Cold and AllergyBrompheniramine maleate (1 mg/5mL) + Phenylephrine hydrochloride (2.5 mg/5mL)SolutionOralAurohealth LLC2015-06-042015-10-13Us
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
BPM Mal Phenyleph HCl DM HBrBrompheniramine maleate (4 mg/5mL) + Dextromethorphan hydrobromide monohydrate (20 mg/5mL) + Phenylephrine hydrochloride (10 mg/5mL)LiquidOralRiver's Edge Pharmaceuticals, LLC2010-01-182012-01-31Us
Brom Mal Phenyl HCl Dex HBrBrompheniramine maleate (4 mg/5mL) + Dextromethorphan hydrobromide monohydrate (15 mg/5mL) + Phenylephrine hydrochloride (7.5 mg/5mL)LiquidOralRiver's Edge Pharmaceuticals, LLC2010-02-102012-02-29Us
BromaxBrompheniramine maleate (11 mg/1)Tablet, extended releaseOralPoly Pharmaceuticals2009-12-012011-11-30Us
Bromdex DBrompheniramine maleate (3 mg/5mL) + Dextromethorphan hydrobromide monohydrate (30 mg/5mL) + Pseudoephedrine hydrochloride (50 mg/5mL)SyrupOralBreckenridge Pharmaceutical, Inc.2009-07-212011-05-31Us
Bromhist PDXBrompheniramine maleate (2 mg/5mL) + Dextromethorphan hydrobromide monohydrate (5 mg/5mL) + Guaifenesin (50 mg/5mL) + Phenylephrine hydrochloride (5 mg/5mL)SyrupOralCypress Pharmaceutical, Inc2006-04-282011-08-26Us
Brompheniramine MaleateBrompheniramine maleate (1 mg/1mL)LiquidOralRiver's Edge Pharmaceuticals, LLC2008-06-012010-10-31Us
Brompheniramine Maleate, Pseudoephedrine Hydrochloride, Dextromethorphan HydrobromideBrompheniramine maleate (4 mg/5mL) + Dextromethorphan hydrobromide monohydrate (20 mg/5mL) + Pseudoephedrine hydrochloride (20 mg/5mL)LiquidOralRiver's Edge Pharmaceuticals, LLC2010-01-182012-01-31Us
Carbofed DMBrompheniramine maleate (4 mg/5mL) + Dextromethorphan hydrobromide monohydrate (15 mg/5mL) + Pseudoephedrine hydrochloride (45 mg/5mL)SyrupOralHi Tech Pharmacal Co., Inc.2001-09-032011-11-03Us
Centussin DhcBrompheniramine maleate (4 mg/5mL) + Dihydrocodeine bitartrate (3 mg/5mL) + Phenylephrine hydrochloride (7.5 mg/5mL)LiquidOralCenturion Labs2009-11-242016-05-02Us
Dihydrocodeine BPM Phenyleph HClBrompheniramine maleate (4 mg/5mL) + Dihydrocodeine bitartrate (3 mg/5mL) + Phenylephrine hydrochloride (7.5 mg/5mL)LiquidOralRiver's Edge Pharmaceuticals, LLC2010-03-012012-02-29Us
International/Other Brands
Bromfed (Wockhardt USA, LLC) / Bromfenex (Ethex Corporation) / Dimetane (Wyeth) / Lodrane (ECR Pharmaceuticals)
Categories
UNII
H57G17P2FN
CAS number
86-22-6
Weight
Average: 319.239
Monoisotopic: 318.073161265
Chemical Formula
C16H19BrN2
InChI Key
ZDIGNSYAACHWNL-UHFFFAOYSA-N
InChI
InChI=1S/C16H19BrN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3
IUPAC Name
[3-(4-bromophenyl)-3-(pyridin-2-yl)propyl]dimethylamine
SMILES
CN(C)CCC(C1=CC=C(Br)C=C1)C1=CC=CC=N1

Pharmacology

Indication

For the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing.

Associated Conditions
Pharmacodynamics

Brompheniramine is an antihistaminergic medication of the propylamine class. It is a first-generation antihistamine. In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Brompheniramine is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.

Mechanism of action

Brompheniramine works by acting as an antagonist of the H1 histamine receptors. It also functions as a moderately effective anticholingeric agent, likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine. Its effects on the cholinergic system may include side-effects such as drowsiness, sedation, dry mouth, dry throat, blurred vision, and increased heart rate.

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption

Antihistamines are well absorbed from the gastrointestinal tract after oral administration.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Hepatic (cytochrome P-450 system), some renal.

Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity

Oral, rat: LD50 = 318 mg/kg. Signs of overdose include fast or irregular heartbeat, mental or mood changes, tightness in the chest, and unusual tiredness or weakness.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Brompheniramine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Brompheniramine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Brompheniramine.
1,10-PhenanthrolineThe therapeutic efficacy of Brompheniramine can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Brompheniramine.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Brompheniramine.
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative and stimulatory activities of Brompheniramine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Brompheniramine.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Brompheniramine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Brompheniramine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with 4-Methoxyamphetamine.
Food Interactions
  • Avoid alcohol.
  • Take with food.

References

Synthesis Reference

Sperber, N., Papa, D. and Schwenk, E.; US. Patent 2,567,245; September 11, 1951; assigned to Schering Corporation. Sperber, N., Papa, D. and Schwenk, E.; U.S. Patent 2,676,964: April 27,1954; assigned to Schering Corporation.

General References
Not Available
External Links
Human Metabolome Database
HMDB0001941
KEGG Drug
D00663
KEGG Compound
C06857
PubChem Compound
6834
PubChem Substance
46508137
ChemSpider
6573
BindingDB
50017666
ChEBI
3183
ChEMBL
CHEMBL811
Therapeutic Targets Database
DAP001066
PharmGKB
PA448675
Drugs.com
Drugs.com Drug Page
Wikipedia
Brompheniramine
ATC Codes
R06AB51 — Brompheniramine, combinationsR06AB01 — Brompheniramine
AHFS Codes
  • 04:04.20 — Propylamine Derivatives
MSDS
Download (73.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentNasal Congestion and Inflammations / Rhinitis1
3WithdrawnTreatmentCoughing / Inflammatory Reaction / Rhinitis1
Not AvailableCompletedTreatmentAllergic Reactions1

Pharmacoeconomics

Manufacturers
  • Alpharma us pharmaceuticals division
  • Kv pharmaceutical co
  • Pharmaceutical assoc inc div beach products
  • Usl pharma inc
  • Watson laboratories inc
  • Wyeth ayerst laboratories
  • Wyeth consumer healthcare
  • Barr laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Newtron pharmaceuticals inc
  • Nexgen pharma inc
  • Par pharmaceutical inc
  • Pioneer pharmaceuticals inc
  • Sandoz inc
  • Vitarine pharmaceuticals inc
Packagers
  • Anip Acquisition Co.
  • Athlon Pharmaceuticals Inc.
  • Boca Pharmacal
  • Brighton Pharmaceuticals
  • C.O. Truxton Inc.
  • Clint Pharmaceutical Inc.
  • Corvit Pharmaceuticals
  • Cypress Pharmaceutical Inc.
  • ECR Pharmaceuticals
  • Elite Laboratories Inc.
  • Great Southern Laboratories
  • Irisys Inc.
  • Jaymac Pharmaceuticals LLC
  • Larken Laboratories Inc.
  • Llorens Pharmaceutical
  • Lunsco Inc.
  • Martica Enterprises Inc.
  • Martin Surgical Supply
  • MCR American Pharmaceuticals Inc.
  • Merit Pharmaceuticals
  • Midlothian Labs
  • Nexgen Pharma Inc.
  • Physicians Total Care Inc.
  • Poly Pharmaceuticals Inc.
  • Provident Pharmaceuticals LLC
  • Quality Care
  • Respa Pharmaceuticals Inc.
  • River's Edge Pharmaceuticals
  • Sovereign Pharmaceuticals Ltd.
  • Spectrum Pharmaceuticals
  • Vision Pharma LLC
  • Wockhardt Ltd.
Dosage forms
FormRouteStrength
Tablet, coatedOral
Tablet, extended releaseOral11 mg/1
LiquidOral1 mg/1mL
SolutionOral
Kit
LiquidIntramuscular; Subcutaneous10 mg
ElixirOral2 mg
TabletOral4 mg
LiquidOral
ElixirOral
Tablet, extended releaseOral
CapsuleOral
Solution / dropsOral
TabletOral
SyrupOral
Tablet, chewableOral
SuspensionOral
Prices
Unit descriptionCostUnit
Brompheniramine maleate powder9.83USD g
Brovex ct 12 mg tablet chew1.58USD tablet
Brompheniramine 12 mg tablet chew1.42USD tablet
Bromfenex-pd capsule sa0.56USD capsule
Bromfed-dm cough syrup0.21USD ml
Brom-pseud-dm syrup0.14USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)< 25 °CPhysProp
boiling point (°C)149.5 °C at 5.00E-01 mm HgPhysProp
water solubilityFreely soluble (maleate salt)Not Available
logP3.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0127 mg/mLALOGPS
logP3.63ALOGPS
logP3.75ChemAxon
logS-4.4ALOGPS
pKa (Strongest Basic)9.48ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area16.13 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity83.67 m3·mol-1ChemAxon
Polarizability32.08 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9648
Blood Brain Barrier+0.9576
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.6242
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.93
Renal organic cation transporterInhibitor0.7955
CYP450 2C9 substrateNon-substrate0.8345
CYP450 2D6 substrateSubstrate0.8346
CYP450 3A4 substrateSubstrate0.5898
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8398
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7748
Ames testNon AMES toxic0.9351
CarcinogenicityNon-carcinogens0.9349
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.0758 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9121
hERG inhibition (predictor II)Inhibitor0.7207
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0002-5490000000-9c3b804de0b552198b85
MS/MS Spectrum - Quattro_QQQ 10V, N/ALC-MS/MSsplash10-014i-4954000000-f0a4889ab8cd0d5dcacc
MS/MS Spectrum - Quattro_QQQ 25V, N/ALC-MS/MSsplash10-00di-0090000000-02a74d4d4927d8e443aa
MS/MS Spectrum - Quattro_QQQ 40V, N/ALC-MS/MSsplash10-014i-0920000000-ad3d20cb0f1b7362fbc3
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as pheniramines. These are compounds containing a pheniramine moiety, which is structurally characterized by the presence of a 2-benzylpyridine linked to an dimethyl(propyl)amine to form a dimethyl[3-phenyl-3-(pyridin-2-yl)propyl]amine skeleton.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Pheniramines
Direct Parent
Pheniramines
Alternative Parents
Bromobenzenes / Aralkylamines / Aryl bromides / Heteroaromatic compounds / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organobromides / Hydrocarbon derivatives
Substituents
Pheniramine / Bromobenzene / Halobenzene / Aralkylamine / Aryl bromide / Benzenoid / Monocyclic benzene moiety / Aryl halide / Heteroaromatic compound / Tertiary aliphatic amine
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
organobromine compound, pyridines (CHEBI:3183)

Targets

Details
1. Histamine H1 receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Bokesoy TA, Onaran HO: Atypical Schild plots with histamine H1 receptor agonists and antagonists in the rabbit aorta. Eur J Pharmacol. 1991 May 2;197(1):49-56. [PubMed:1680053]
  2. Onaran HO, Bokesoy TA: Kinetics of antagonism at histamine-H1 receptors in isolated rabbit arteries. Naunyn Schmiedebergs Arch Pharmacol. 1990 Apr;341(4):316-23. [PubMed:1970615]
  3. Yanni JM, Stephens DJ, Parnell DW, Spellman JM: Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular use. J Ocul Pharmacol. 1994 Winter;10(4):665-75. [PubMed:7714410]
  4. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [PubMed:7855217]
  5. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Yasuda SU, Yasuda RP: Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [PubMed:10212017]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on December 12, 2018 07:09