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Identification
NameErgoloid mesylate
Accession NumberDB01049  (APRD00711, DB01287)
TypeSmall Molecule
GroupsApproved
Description

Ergoloid mesylate is a dihydrogenated ergot (Claviceps purpurea) derivative alkaloid used as a vasodilator agent. Ergoloid Mesylate is the only vasodilator that has shown mild benefits in the treatment of vascular dementia. Ergoloid Mesylate is a mixture of three different ergotamantriones: dihydroergocornine, dihydroergocristine, and dihydroergocryptine. It has been proposed to be a neuroprotective agent. The mechanism of its therapeutic actions is not clear.

Structure
Thumb
Synonyms
co-dergocrine mesilate
co-dergocrine mesylate
co-dergocrine methanesulfonate
codergocrine mesilate
codergocrine mesylate
codergocrine methanesulfonate
Dihydroergotoxine Mesilate
Dihydroergotoxine Mesylate
dihydroergotoxine methanesulfonate
Dihydroergotoxine Methanesulfonate
dihydroergotoxine methanesulfonates
dihydroergotoxine monomethanesulfonate
dihydrogenated ergot alkaloids
Ergoloid Mesylates
ergoloid methanesulfonate
ergoloid methanesulfonates
hydrogenated ergot alkaloids
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Hydergine Tablets, 1mgtablet1 mgoralSterimax Inc1968-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlkergotNot Available
GerimalNot Available
HydergineNot Available
Hydergine LCNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIX3S33EX3KW
CAS number8067-24-1
WeightAverage: 631.74
Monoisotopic: 631.267584003
Chemical FormulaC30H41N5O8S
InChI KeyInChIKey=FQHMMOGHDWAXDI-WUQHHHCFSA-N
InChI
InChI=1S/C29H37N5O5.CH4O3S/c1-15(2)28(27(37)34-16(3)26(36)33-10-6-9-23(33)29(34,38)39-28)31-25(35)18-11-20-19-7-5-8-21-24(19)17(13-30-21)12-22(20)32(4)14-18;1-5(2,3)4/h5,7-8,13,15-16,18,20,22-23,30,38H,6,9-12,14H2,1-4H3,(H,31,35);1H3,(H,2,3,4)/t16-,18+,20+,22+,23-,28+,29-;/m0./s1
IUPAC Name
(2R,4R,7R)-N-[(1S,2S,4R,7S)-2-hydroxy-7-methyl-5,8-dioxo-4-(propan-2-yl)-3-oxa-6,9-diazatricyclo[7.3.0.0²,⁶]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0²,⁷.0¹²,¹⁶]hexadeca-1(16),9,12,14-tetraene-4-carboxamide; methanesulfonic acid
SMILES
CS(O)(=O)=O.[H][C@@]12CCCN1C(=O)[[email protected]](C)N1C(=O)[C@](NC(=O)[[email protected]]3CN(C)[C@]4([H])CC5=CNC6=CC=CC(=C56)[C@@]4([H])C3)(O[C@@]21O)C(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as ergopeptines. These are ergoline derivatives that contain a tripeptide structure attached to the basic ergoline ring in the same location as the amide group of the lysergic acid derivatives.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassErgoline and derivatives
Sub ClassLysergic acids and derivatives
Direct ParentErgopeptines
Alternative Parents
Substituents
  • Hybrid peptide
  • Ergopeptine
  • Lysergic acid amide
  • Indoloquinoline
  • Benzoquinoline
  • Quinoline-3-carboxamide
  • Pyrroloquinoline
  • N-acyl-alpha amino acid or derivatives
  • Quinoline
  • Piperidinecarboxylic acid
  • Piperidinecarboxamide
  • 3-piperidinecarboxamide
  • Isoindole or derivatives
  • Indole or derivatives
  • Indole
  • Aralkylamine
  • N-alkylpiperazine
  • Benzenoid
  • Piperidine
  • Piperazine
  • Oxazolidinone
  • 1,4-diazinane
  • Heteroaromatic compound
  • Alkanesulfonic acid
  • Tertiary carboxylic acid amide
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonic acid
  • Pyrrolidine
  • Pyrrole
  • Methanesulfonate
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Orthocarboxylic acid derivative
  • Lactam
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Alkanolamine
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
  • Aliphatic acyclic compound
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor use as an adjunct therapy for patients with dementia.
PharmacodynamicsErgoloid Mesylate may increase cerebral metabolism and blood flow. The role of this medication in the therapy of dementia is controversial. A recent controlled study in patients with Alzheimer's disease found that there was no advantage to the use of ergoloid mesylates compared to placebo, suggesting that ergoloid mesylates may lower scores on some cognitive and behavioral rating scales. Further study is needed to determine the risk-benefit profile of ergoloid mesylates in the treatment of dementia.
Mechanism of actionErgoloid mesylates act centrally, decreasing vascular tone and slowing the heart rate, and acts peripherally to block alpha-receptors. One other possible mechanism is the effect of ergoloid mesylates on neuronal cell metabolism, resulting in improved oxygen uptake and cerebral metabolism, thereby normalizing depressed neurotransmitter levels.
Related Articles
AbsorptionRapidly but incompletely (approximately 25%) absorbed from the gastrointestinal tract. Approximately 50% of the absorbed dose is eliminated by first-pass metabolism.
Volume of distributionNot Available
Protein binding98-99%
Metabolism

Hepatic.

Route of eliminationNot Available
Half life3.5 hours
ClearanceNot Available
ToxicitySymptoms of overdose include dyspnea, hypotension or hypertension, rapid weak pulse, delirium, nausea, vomiting, and bradycardia.
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+0.8284
Blood Brain Barrier-0.9494
Caco-2 permeable-0.6447
P-glycoprotein substrateSubstrate0.6838
P-glycoprotein inhibitor IInhibitor0.6581
P-glycoprotein inhibitor IINon-inhibitor0.8001
Renal organic cation transporterNon-inhibitor0.8838
CYP450 2C9 substrateNon-substrate0.75
CYP450 2D6 substrateNon-substrate0.7966
CYP450 3A4 substrateSubstrate0.6681
CYP450 1A2 substrateNon-inhibitor0.7702
CYP450 2C9 inhibitorNon-inhibitor0.7072
CYP450 2D6 inhibitorNon-inhibitor0.9221
CYP450 2C19 inhibitorNon-inhibitor0.6493
CYP450 3A4 inhibitorNon-inhibitor0.7973
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8464
Ames testNon AMES toxic0.6324
CarcinogenicityNon-carcinogens0.6535
BiodegradationNot ready biodegradable0.9321
Rat acute toxicity2.5438 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8821
hERG inhibition (predictor II)Inhibitor0.5783
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg
Prices
Unit descriptionCostUnit
Ergoloid mesylates powder87.5USD g
Ergoloid mesylates 1 mg tablet1.3USD tablet
Hydergine 1 mg Tablet1.1USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP2.8Not Available
Predicted Properties
PropertyValueSource
logP2.17ChemAxon
pKa (Strongest Acidic)9.71ChemAxon
pKa (Strongest Basic)8.39ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area118.21 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity143.66 m3·mol-1ChemAxon
Polarizability57.99 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesC04AE51C04AE01
AHFS Codes
  • 12:16.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (72.9 KB)
Interactions
Drug Interactions
Drug
AcepromazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Acetophenazine.
AmisulprideThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Amisulpride.
AprepitantThe serum concentration of Ergoloid mesylate can be increased when it is combined with Aprepitant.
AripiprazoleThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Aripiprazole.
BatimastatThe serum concentration of Ergoloid mesylate can be increased when it is combined with Batimastat.
BenzquinamideThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Benzquinamide.
BoceprevirThe serum concentration of Ergoloid mesylate can be increased when it is combined with Boceprevir.
CarphenazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Carphenazine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Chlorprothixene.
ClarithromycinThe serum concentration of Ergoloid mesylate can be increased when it is combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Clozapine.
ConivaptanThe serum concentration of Ergoloid mesylate can be increased when it is combined with Conivaptan.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Ergoloid mesylate.
DasatinibThe serum concentration of Ergoloid mesylate can be increased when it is combined with Dasatinib.
DroperidolThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Droperidol.
EletriptanErgoloid mesylate may increase the vasoconstricting activities of Eletriptan.
FencamfamineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Fencamfamine.
FluconazoleThe metabolism of Ergoloid mesylate can be decreased when combined with Fluconazole.
FlupentixolThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Ergoloid mesylate.
FosaprepitantThe serum concentration of Ergoloid mesylate can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Ergoloid mesylate can be increased when it is combined with Fusidic Acid.
GranisetronGranisetron may increase the serotonergic activities of Ergoloid mesylate.
HaloperidolThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Haloperidol.
IdelalisibThe serum concentration of Ergoloid mesylate can be increased when it is combined with Idelalisib.
IsoflurophateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Isoflurophate.
ItraconazoleThe serum concentration of Ergoloid mesylate can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Ergoloid mesylate can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Ergoloid mesylate can be increased when it is combined with Ketoconazole.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergoloid mesylate.
LoxapineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Loxapine.
LuliconazoleThe serum concentration of Ergoloid mesylate can be increased when it is combined with Luliconazole.
MesoridazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Methotrimeprazine.
MetoclopramideThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Metoclopramide.
MifepristoneThe serum concentration of Ergoloid mesylate can be increased when it is combined with Mifepristone.
MolindoneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Molindone.
NadololNadolol may increase the vasoconstricting activities of Ergoloid mesylate.
NelfinavirThe metabolism of Ergoloid mesylate can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Ergoloid mesylate can be increased when it is combined with Netupitant.
NitroglycerinErgoloid mesylate may decrease the vasodilatory activities of Nitroglycerin.
OlanzapineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Ondansetron.
PalbociclibThe serum concentration of Ergoloid mesylate can be increased when it is combined with Palbociclib.
PaliperidoneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Paliperidone.
PerphenazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Perphenazine.
PimozideThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Piperacetazine.
PosaconazoleThe serum concentration of Ergoloid mesylate can be increased when it is combined with Posaconazole.
ProchlorperazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Risperidone.
SertindoleThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Sertindole.
SimeprevirThe serum concentration of Ergoloid mesylate can be increased when it is combined with Simeprevir.
StiripentolThe serum concentration of Ergoloid mesylate can be increased when it is combined with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Sulpiride.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Ergoloid mesylate.
TelaprevirThe serum concentration of Ergoloid mesylate can be increased when it is combined with Telaprevir.
ThioridazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Thiothixene.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Ergoloid mesylate.
TrifluoperazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Triflupromazine.
VoriconazoleThe serum concentration of Ergoloid mesylate can be increased when it is combined with Voriconazole.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol.
Components:
NameUniProt IDDetails
Alpha-2A adrenergic receptorP08913 Details
Alpha-2B adrenergic receptorP18089 Details
Alpha-2C adrenergic receptorP18825 Details
References
  1. Markstein R: Hydergine: interaction with the neurotransmitter systems in the central nervous system. J Pharmacol. 1985;16 Suppl 3:1-17. [PubMed:2869188 ]
Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Components:
NameUniProt IDDetails
Alpha-1A adrenergic receptorP35348 Details
Alpha-1B adrenergic receptorP35368 Details
Alpha-1D adrenergic receptorP25100 Details
References
  1. Markstein R: Hydergine: interaction with the neurotransmitter systems in the central nervous system. J Pharmacol. 1985;16 Suppl 3:1-17. [PubMed:2869188 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Lu WJ, Huang JD, Lai ML: The effects of ergoloid mesylates and ginkgo biloba on the pharmacokinetics of ticlopidine. J Clin Pharmacol. 2006 Jun;46(6):628-34. [PubMed:16707409 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli.
Components:
NameUniProt IDDetails
5-hydroxytryptamine receptor 1AP08908 Details
5-hydroxytryptamine receptor 1BP28222 Details
5-hydroxytryptamine receptor 1DP28221 Details
5-hydroxytryptamine receptor 1EP28566 Details
5-hydroxytryptamine receptor 1FP30939 Details
5-hydroxytryptamine receptor 2AP28223 Details
5-hydroxytryptamine receptor 2BP41595 Details
5-hydroxytryptamine receptor 2CP28335 Details
5-hydroxytryptamine receptor 3AP46098 Details
5-hydroxytryptamine receptor 3BO95264 Details
5-hydroxytryptamine receptor 3CQ8WXA8 Details
5-hydroxytryptamine receptor 3DQ70Z44 Details
5-hydroxytryptamine receptor 3EA5X5Y0 Details
5-hydroxytryptamine receptor 4Q13639 Details
5-hydroxytryptamine receptor 6P50406 Details
5-hydroxytryptamine receptor 7P34969 Details
References
  1. Flynn BL, Ranno AE: Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97. [PubMed:10084415 ]
  2. Markstein R: Hydergine: interaction with the neurotransmitter systems in the central nervous system. J Pharmacol. 1985;16 Suppl 3:1-17. [PubMed:2869188 ]
  3. Wadworth AN, Chrisp P: Co-dergocrine mesylate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in age-related cognitive decline. Drugs Aging. 1992 May-Jun;2(3):153-73. [PubMed:1606351 ]
  4. Korneyev AY, Cincotta AH: Identification of hepatic, non-monoamine, dihydroergocryptine binding sites with significant gender differences. Life Sci. 1996;58(12):241-8. [PubMed:8786706 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonistagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Flynn BL, Ranno AE: Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97. [PubMed:10084415 ]
  2. Markstein R: Hydergine: interaction with the neurotransmitter systems in the central nervous system. J Pharmacol. 1985;16 Suppl 3:1-17. [PubMed:2869188 ]
  3. Wadworth AN, Chrisp P: Co-dergocrine mesylate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in age-related cognitive decline. Drugs Aging. 1992 May-Jun;2(3):153-73. [PubMed:1606351 ]
  4. Korneyev AY, Cincotta AH: Identification of hepatic, non-monoamine, dihydroergocryptine binding sites with significant gender differences. Life Sci. 1996;58(12):241-8. [PubMed:8786706 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonistagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Markstein R: Hydergine: interaction with the neurotransmitter systems in the central nervous system. J Pharmacol. 1985;16 Suppl 3:1-17. [PubMed:2869188 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Components:
NameUniProt IDDetails
Gamma-aminobutyric acid receptor subunit alpha-1P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3P28472 Details
Gamma-aminobutyric acid receptor subunit deltaO14764 Details
Gamma-aminobutyric acid receptor subunit epsilonP78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3Q99928 Details
Gamma-aminobutyric acid receptor subunit piO00591 Details
Gamma-aminobutyric acid receptor subunit thetaQ9UN88 Details
References
  1. Tvrdeic A, Pericic D: Effect of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors. Coll Antropol. 2003;27 Suppl 1:175-82. [PubMed:12955907 ]
  2. Tvrdeic A, Pericic D: Dihydrogenated ergot compounds bind with high affinity to GABAA receptor-associated Cl- ionophore. Eur J Pharmacol. 1991 Sep 4;202(1):109-11. [PubMed:1664802 ]
  3. Korneyev AY, Cincotta AH: Identification of hepatic, non-monoamine, dihydroergocryptine binding sites with significant gender differences. Life Sci. 1996;58(12):241-8. [PubMed:8786706 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Althaus M, Retzow A, Castell JV, Gomez-Lechon MJ, Amalou Z, Rose T, Appel K: In vitro identification of the cytochrome P450 isoform responsible for the metabolism of alpha-dihydroergocryptine. Xenobiotica. 2000 Nov;30(11):1033-45. [PubMed:11197065 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23