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Identification
NameHyoscyamine
Accession NumberDB00424  (APRD00607)
TypeSmall Molecule
GroupsApproved
Description

Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.)
Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson’s disease, as well as for control of respiratory secretions in end of life care.

Structure
Thumb
Synonyms
(-)-Atropine
(-)-Hyoscyamine
(−)-atropine
(−)-hyoscyamine
(S)-(-)-Hyoscyamine
(S)-(−)-hyoscyamine
(S)-atropine
[3(S)-Endo]-alpha-(hydroxymethyl)benzeneacetic acid 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
Daturin
Daturine
Duboisine
Hyoscyamin
Hyoscyamine
Hyoscyaminum
L-Hyoscyamine
L-Tropine Tropate
Tropine-L-tropate
Tropine, (-)-tropate
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Levsintablet0.125 mgoralSchwarz Pharma Kremers Urban Company1960-12-312008-08-08Canada
Levsin Drops 0.125mg/mldrops0.125 mgoralSchwarz Pharma Kremers Urban Company1982-12-311996-09-09Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Anaspaztablet, orally disintegrating.125 mg/1oral; sublingualBF ASCHER AND CO INC1973-01-02Not applicableUs
Direct Rxtablet.125 mg/1oralDIRECT RX2015-01-01Not applicableUs
Ed-spaztablet, orally disintegrating.125 mg/1oralEDWARDS PHARMACEUTICALS, INC.2010-05-12Not applicableUs
Hyoscyamineliquid.125 mg/5mLoralPatrin Pharma2011-09-04Not applicableUs
Hyoscyamineliquid.125 mg/mLoralPatrin Pharma2011-09-04Not applicableUs
Hyoscyaminetablet.125 mg/1oralWallace Pharmaceuticals Inc.2016-04-01Not applicableUs
Hyoscyamine Sltablet, orally disintegrating.125 mg/1oralWallace Pharmaceuticals Inc.2016-04-15Not applicableUs
Hyoscyamine Sulfateelixir.125 mg/5mLoralCypress Pharmaceutical, Inc.2008-11-21Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralVirtus Pharmaceuticals2011-09-04Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oral; sublingualCounty Line Pharmaceuticals, LLC2009-09-21Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oral; sublingualbryant ranch prepack2009-09-21Not applicableUs
Hyoscyamine Sulfatesolution.125 mg/mLoralMethod Pharmaceuticals, Llc2014-12-01Not applicableUs
Hyoscyamine Sulfatetablet, orally disintegrating.125 mg/1oralVirtus Pharmaceuticals2011-09-04Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralAidarex Pharmaceuticals LLC2009-11-05Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oral; sublingualPd Rx Pharmaceuticals, Inc.2009-09-21Not applicableUs
Hyoscyamine Sulfatetablet, orally disintegrating.125 mg/1oralAvera Mc Kennan Hospital2015-03-04Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oral; sublingualCarilion Materials Management2009-09-21Not applicableUs
Hyoscyamine Sulfatetablet.375 mg/1oralFranklin Pharmaceutical LLC2010-05-01Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralProficient Rx LP2009-11-05Not applicableUs
Hyoscyamine Sulfateelixir.125 mg/5mLoralMethod Pharmaceuticals, Llc2014-11-01Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralPreferred Pharmaceuticals Inc.2015-10-27Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oral; sublingualProficient Rx LP2009-09-21Not applicableUs
Hyoscyamine Sulfatetablet.375 mg/1oralClinical Solutions Wholesale2009-11-05Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralFranklin Pharmaceutical LLC2010-05-01Not applicableUs
Hyoscyamine Sulfatetablet.375 mg/1oralKmr Pharmaceuticals Llc2011-01-01Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oral; sublingualRebel Distributors Corp2009-09-21Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralKmr Pharmaceuticals Llc2011-01-01Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralKmr Pharmaceuticals Llc2011-01-01Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralCounty Line Pharmaceuticals, LLC2009-11-05Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralRebel Distributors Corp2009-11-05Not applicableUs
Hyoscyamine Sulfatesolution/ drops.125 mg/mLoralCypress Pharmaceutical, Inc.2008-12-30Not applicableUs
Hyoscyamine Sulfatetablet.125 mg/1oralKmr Pharmaceuticals Llc2011-01-01Not applicableUs
Hyoscyamine Sulfatetablet, orally disintegrating.125 mg/1oralCounty Line Pharmaceuticals, LLC2009-09-21Not applicableUs
Hyoscyamine Sulfate Extended-releasetablet.375 mg/1oralCarilion Materials Management2010-01-03Not applicableUs
Hyoscyamine Sulfate Extended-releasetablet.375 mg/1oralAidarex Pharmaceuticals LLC2010-01-03Not applicableUs
Hyoscyamine Sulfate Extended-releasetablet.375 mg/1oralCounty Line Pharmaceuticals, LLC2010-01-03Not applicableUs
Hyoscyamine Sulfate Extended-releasetablet.375 mg/1oralAmerican Health Packaging2015-03-31Not applicableUs
Hyoscyamine Sulfate Sltablet.125 mg/1oralVirtus Pharmaceuticals2011-09-04Not applicableUs
Hyoscyamine Sulfate Sltablet, soluble.125 mg/1oralFranklin Pharmaceutical LLC2010-05-01Not applicableUs
Hyoscyamine Sulfate Sltablet.125 mg/1oralREMEDYREPACK INC.2015-08-07Not applicableUs
Hyosyneelixir.125 mg/5mLoralSilarx Pharmaceuticals, Inc1997-11-01Not applicableUs
Hyosynesolution/ drops.125 mg/mLoralSilarx Pharmaceuticals, Inc1997-10-01Not applicableUs
Levbidtablet.375 mg/1oralAlaven Pharmaceutical LLC2008-12-01Not applicableUs
Levsininjection, solution.5 mg/mLsubcutaneousAlaven Pharmaceutical LLC2008-12-01Not applicableUs
Levsintablet.125 mg/1oralAlaven Pharmaceutical LLC1955-06-01Not applicableUs
Levsin Sltablet, orally disintegrating.125 mg/1oralAlaven Pharmaceutical LLC2008-12-01Not applicableUs
Nulevtablet, chewable.125 mg/1oralAlaven Pharmaceutical LLC2008-12-01Not applicableUs
Oscimintablet, extended release.375 mg/1oralLarken Laboratories, Inc.2011-08-03Not applicableUs
Oscimintablet, orally disintegrating.125 mg/1oralLarken Laboratories, Inc.2011-08-03Not applicableUs
Oscimintablet, orally disintegrating.125 mg/1sublingualLarken Laboratories, Inc.2011-08-03Not applicableUs
Oscimintablet.125 mg/1oralLarken Laboratories, Inc.2011-08-03Not applicableUs
Symax Duotabtablet, multilayer, extended release.375 mg/1oralCapellon Pharmaceuticals, LLC2009-11-07Not applicableUs
Symax Fastabtablet, orally disintegrating.125 mg/1oralCapellon Pharmaceuticals, LLC2003-11-012015-12-29Us
Symax Sltablet, orally disintegrating.125 mg/1oralCapellon Pharmaceuticals, LLC1996-09-01Not applicableUs
Symax SRtablet, extended release.375 mg/1oralCapellon Pharmaceuticals, LLC2009-11-07Not applicableUs
International Brands
NameCompany
AcupazGlitz
AnapazHilton
AnaspazAscher
AtropenNot Available
Boots Travel CalmBoots
BuweconYung Shin
CystospazNot Available
CytospazAmerifit
DonnamarNot Available
EgazilBioPhausia
LevbidNot Available
LevsinexNot Available
NuLevNot Available
SymaxCapellon
Brand mixtures
NameLabellerIngredients
Azuphen MbBurel Pharmaceuticals, Inc
B-donnaWinder Laboratories, LLC
Belladonna Alkaloids With PhenobartbitalLiberty Pharmaceuticals, Inc.
Calmitol Itching Relief OntPfizer Canada Inc., Consumer Healthcare Division
Diban CapAyerst Laboratories
Donnagel LiqAyerst Laboratories
DonnatalKAISER FOUNDATION HOSPITALS
Donnatal ElixirAyerst Laboratories
Donnatal ExtentabsPBM Pharmaceuticals, Inc
Donnatal Extentabs SrtWyeth Ayerst Canada Inc.
Donnatal TabWyeth Ayerst Canada Inc.
Hyolev MbBurel Pharmaceuticals, Inc
HyophenStar Pharmaceuticals, Llc
Indiomin MbBurel Pharmaceuticals, Inc
Me Naphos Mb Hyo 1Method Pharmaceuticals
Me-PB-hyosMethod Pharmaceuticals, Llc
PhenohytroWinder Laboratories, LLC
PhosphasalStar Pharmaceuticals, Llc
QuadrapaxRebel Distributors Corp
Re-PB Hyos ElixirKAISER FOUNDATION HOSPITALS
Se-donna Pb HyosSeton Pharmaceuticals
Ur N-C Urinary AntisepticLibertas Pharma, Inc.
UralgicWestminster
Uramit MbBurel Pharmaceuticals, Inc
UrelleMeda Pharmaceuticals Inc.
UribelStar Pharmaceuticals, Llc
Urimar-TMarnel Pharmaceutical, Inc.
Urin D/sLlorens Pharmaceutical International Division
Uro-LMethod Pharmaceuticals, Llc
Uro-MPMethod Pharmaceuticals, Llc
Uroav-81Av Kare, Inc.
Uroav-BAv Kare, Inc.
Urogesic BlueEdwards Pharmaceutical, Inc.
Urolet MbBurel Pharmaceuticals, Inc
Urophen MbBurel Pharmaceuticals, Inc
UstellStar Pharmaceuticals Llc
UtaSj Pharmaceuticals, Llc
Utira-CMission Pharmacal Company
Salts
Name/CASStructureProperties
Hyoscyamine hydrobromide
ThumbNot applicableDBSALT001048
Hyoscyamine sulfate
620-61-1
ThumbNot applicableDBSALT001011
Categories
UNIIPX44XO846X
CAS number101-31-5
WeightAverage: 289.3694
Monoisotopic: 289.167793607
Chemical FormulaC17H23NO3
InChI KeyInChIKey=RKUNBYITZUJHSG-FXUDXRNXSA-N
InChI
InChI=1S/C17H23NO3/c1-18-13-7-8-14(18)10-15(9-13)21-17(20)16(11-19)12-5-3-2-4-6-12/h2-6,13-16,19H,7-11H2,1H3/t13-,14+,15+,16-/m1/s1
IUPAC Name
(1R,3R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl (2S)-3-hydroxy-2-phenylpropanoate
SMILES
CN1[[email protected]]2CC[C@@H]1C[C@@H](C2)OC(=O)[[email protected]](CO)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylacetic acid derivatives. These are compounds containing a phenylacetic acid moiety, which consists of a phenyl group substituted at the second position by an acetic acid.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylacetic acid derivatives
Direct ParentPhenylacetic acid derivatives
Alternative Parents
Substituents
  • Phenylacetate
  • Tropane alkaloid
  • Beta-hydroxy acid
  • N-alkylpyrrolidine
  • Piperidine
  • Hydroxy acid
  • Pyrrolidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid ester
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor treatment of bladder spasms, peptic ulcer disease, diverticulitis, colic, irritable bowel syndrome, cystitis, and pancreatitis. Also used to treat certain heart conditions, to control the symptoms of Parkinson's disease and rhinitis.
PharmacodynamicsL-Hyoscyamine, the active optical isomer of atropine (dl-hyoscyamine), is a tertiary amine anticholinergic gastrointestinal agent.
Mechanism of actionHyoscyamine competes favorably with acetylcholine for binding at muscarinic receptors in the salivary, bronchial, and sweat glands as well as in the eye, heart, and gastrointestinal tract. The actions of hyoscyamine result in a reduction in salivary, bronchial, gastric and sweat gland secretions, mydriasis, cycloplegia, change in heart rate, contraction of the bladder detrusor muscle and of the gastrointestinal smooth muscle, and decreased gastrointestinal motility.
Related Articles
AbsorptionAbsorbed totally and completely by sublingual administration as well as oral administration.
Volume of distributionNot Available
Protein binding50%
Metabolism

Hepatic

Route of eliminationNot Available
Half life2-3.5 hours
ClearanceNot Available
ToxicitySymptoms of overdose include headache, nausea, vomiting, blurred vision, dilated pupils, hot dry skin, dizziness, dryness of the mouth, difficulty in swallowing, and CNS stimulation. LD50=mg/kg(orally in rat)
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9286
Blood Brain Barrier+0.9569
Caco-2 permeable+0.8866
P-glycoprotein substrateSubstrate0.5
P-glycoprotein inhibitor INon-inhibitor0.6542
P-glycoprotein inhibitor IINon-inhibitor0.8595
Renal organic cation transporterInhibitor0.7956
CYP450 2C9 substrateNon-substrate0.7041
CYP450 2D6 substrateNon-substrate0.6838
CYP450 3A4 substrateSubstrate0.5496
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9275
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9285
CYP450 3A4 inhibitorNon-inhibitor0.95
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9113
Ames testNon AMES toxic0.7742
CarcinogenicityNon-carcinogens0.9631
BiodegradationReady biodegradable0.5527
Rat acute toxicity2.7305 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8354
hERG inhibition (predictor II)Inhibitor0.5378
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tablet, orally disintegratingoral; sublingual.125 mg/1
Ointmenttopical
Liquidoral
Tablet (extended-release)oral
Tablet, film coated, extended releaseoral
Tablet, orally disintegratingoral.125 mg/1
Liquidoral.125 mg/5mL
Liquidoral.125 mg/mL
Solutionoral.125 mg/mL
Tabletoral.125 mg/1
Tabletoral; sublingual.125 mg/1
Tabletoral.375 mg/1
Tablet, solubleoral.125 mg/1
Elixiroral.125 mg/5mL
Solution/ dropsoral.125 mg/mL
Injection, solutionsubcutaneous.5 mg/mL
Tabletoral0.125 mg
Dropsoral0.125 mg
Tablet, chewableoral.125 mg/1
Tablet, orally disintegratingsublingual.125 mg/1
Elixiroral
Tablet, multilayer, extended releaseoral.375 mg/1
Tablet, extended releaseoral.375 mg/1
Tabletoral
Capsuleoral
Tablet, coatedoral
Prices
Unit descriptionCostUnit
Levsin 0.125 mg/ml Solution 15ml Bottle49.09USD bottle
Levsin 0.5 mg/ml ampul27.33USD ml
Hyoscyamine sulfate powder25.69USD g
Symax Duotab 0.375 mg Controlled Release Tabs3.73USD tab
Symax-SL 0.125 mg Sublingual Tabs3.29USD tab
Symax duotab2.4USD tablet
Levbid 0.375 mg 12 Hour tablet2.12USD tablet
Levbid er 0.375 mg tablet2.09USD tablet
Hyoscyamine Sulfate CR 0.375 mg 12 Hour tablet1.66USD tablet
Levbid 0.375 mg tablet sa1.44USD tablet
Symax-sr 0.375 mg tablet1.4USD tablet
Levsin/SL 0.125 mg Sublingual Tabs1.24USD tab
Symax fastabs 0.125 mg tablet1.21USD tablet
Symax-sl 0.125 mg tablet sl1.17USD tablet
Levsin 0.125 mg tablet1.08USD tablet
Levsin-sl 0.125 mg tablet sl0.97USD tablet
Hyoscyamine Sulfate 0.125 mg tablet0.93USD tablet
Nulev 0.125 mg tablet0.91USD tablet
Hyoscyamine Sulfate 0.125 mg Sublingual Tabs0.88USD tab
Hyomax-sl 0.125 mg tablet sl0.86USD tablet
Hyoscyamine Sulfate 0.125 mg Dispersible Tablet0.83USD dispersible tablet
Hyoscyamine sulf 0.125 mg tablet0.79USD tablet
Hyoscyamine su 0.125 mg tablet0.64USD tablet
Hyoscyamine 0.125 mg tablet sl0.53USD tablet
Hyoscyamine sul 0.15 mg tablet sl0.39USD tablet
Anaspaz 0.125 mg Dispersible Tablet0.36USD dispersible tablet
Levsin 0.125 mg/5ml Elixir0.29USD ml
Anaspaz 0.125 mg tablet sl0.26USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point108.5 °CPhysProp
water solubility3560 mg/L (at 20 °C)MERCK INDEX (1996); pH 9.5
logP1.8Not Available
logS-1.91ADME Research, USCD
pKa11.7MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility2.52 mg/mLALOGPS
logP2.19ALOGPS
logP1.57ChemAxon
logS-2.1ALOGPS
pKa (Strongest Acidic)15.15ChemAxon
pKa (Strongest Basic)9.39ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area49.77 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity80.82 m3·mol-1ChemAxon
Polarizability31.74 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.14 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-00di-9810000000-bdd60b3a23f97899d426View in MoNA
1D NMR1H NMR SpectrumNot Available
1D NMR13C NMR SpectrumNot Available
References
Synthesis Reference

Jeffrey Kiel, H. Thomas, Emily Ware, Brady Ware, “Phenolic acid complexes of hyoscyamine and process for preparing the same.” U.S. Patent US20060128637, issued June 15, 2006.

US20060128637
General ReferencesNot Available
External Links
ATC CodesA03BA03A03CB31
AHFS Codes
  • 12:08.08
  • 92:02.00*
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.4 KB)
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Hyoscyamine.
Aluminum hydroxideThe serum concentration of Hyoscyamine can be decreased when it is combined with Aluminum hydroxide.
Botulinum Toxin Type AHyoscyamine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BHyoscyamine may increase the anticholinergic activities of Botulinum Toxin Type B.
Calcium carbonateThe serum concentration of Hyoscyamine can be decreased when it is combined with Calcium carbonate.
Cimetropium BromideHyoscyamine may increase the anticholinergic activities of Cimetropium Bromide.
DronabinolHyoscyamine may increase the tachycardic activities of Dronabinol.
EluxadolineHyoscyamine may increase the activities of Eluxadoline.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Glucagon recombinant.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Hyoscyamine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Hyoscyamine.
Magnesium hydroxideThe serum concentration of Hyoscyamine can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Hyoscyamine can be decreased when it is combined with Magnesium oxide.
MianserinMianserin may increase the anticholinergic activities of Hyoscyamine.
MirabegronThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Mirabegron.
MorphineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Morphine.
Potassium ChlorideHyoscyamine may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Hyoscyamine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Hyoscyamine.
RamosetronHyoscyamine may increase the activities of Ramosetron.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Hyoscyamine.
Sodium bicarbonateThe serum concentration of Hyoscyamine can be decreased when it is combined with Sodium bicarbonate.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Hyoscyamine.
TacrineThe therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Tacrine.
TiotropiumHyoscyamine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Topiramate.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Hyoscyamine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Hyoscyamine.
Food Interactions
  • Take 30 minutes before meals, and at bedtime.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Huang XP, Williams FE, Peseckis SM, Messer WS Jr: Pharmacological characterization of human m1 muscarinic acetylcholine receptors with double mutations at the junction of TM VI and the third extracellular domain. J Pharmacol Exp Ther. 1998 Sep;286(3):1129-39. [PubMed:9732369 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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 action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Lysikova M, Havlas Z, Tucek S: Interactions between allosteric modulators and 4-DAMP and other antagonists at muscarinic receptors: potential significance of the distance between the N and carboxyl C atoms in the molecules of antagonists. Neurochem Res. 2001 Apr;26(4):383-94. [PubMed:11495349 ]
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Lysikova M, Havlas Z, Tucek S: Interactions between allosteric modulators and 4-DAMP and other antagonists at muscarinic receptors: potential significance of the distance between the N and carboxyl C atoms in the molecules of antagonists. Neurochem Res. 2001 Apr;26(4):383-94. [PubMed:11495349 ]
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 action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 Da
References
  1. Lysikova M, Havlas Z, Tucek S: Interactions between allosteric modulators and 4-DAMP and other antagonists at muscarinic receptors: potential significance of the distance between the N and carboxyl C atoms in the molecules of antagonists. Neurochem Res. 2001 Apr;26(4):383-94. [PubMed:11495349 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on February 10, 2016 10:12