Identification
- Summary
Pizotifen is a serotonin and tryptamine antagonist indicated for migraine prophylaxis.
- Brand Names
- Sandomigran
- Generic Name
- Pizotifen
- DrugBank Accession Number
- DB06153
- Background
Pizotifen belongs to the class of antamines and is related to cyproheptadine.1 It is a potent serotonin and tryptamine antagonist that has been used for migraine prevention for many years. It exhibits weak anticholinergic, antihistamine, and antikinin actions in addition to sedative and appetite-stimulating properties 10. Some patients receiving pizotifen treatment developed tolerance with the prolonged use of the drug 10. Numerous studies have revealed the potential antidepressant effects of pizotifen, which are independent of its antimigraine action 5. While it is suggested that pizotifen may act similarly to the classic tricyclic antidepressants 5, its full mechanism of antidepressant action is not fully elucidated. Pizotifen hydrochloride is an active ingredient in Sandomigran, which is used for the prophylactic management of migraines. Sandomigran is available in a number of countries but is not approved by the FDA nor EMA.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Pizotifen (DB06153)
- Weight
- Average: 295.44
Monoisotopic: 295.139470854 - Chemical Formula
- C19H21NS
- Synonyms
- Pizotifen
- pizotifeno
- Pizotyline
- External IDs
- BC-105
Pharmacology
- Indication
Indicated for the prophylactic management of migraines 10.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prophylaxis of Migraine •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Various studies have shown pizotifen to be effective in the prophylaxis of migraines in reducing the frequency and severity of vascular headaches 3. Evidence from studies in vivo and in vitro demonstrate antagonistic actions towards serotonin and histamine. Pizotifen blocks the postsynaptic 5-HT2 receptors, as supported by antagonism of several direct agonists of 5-HT receptors 5. It is an antagonist at histamine H1 receptors, and is weakly anticholinergic 9. It also binds to α1- and α2-adrenergic receptors, and dopamine receptors 9. Pizotifen elicits a minimal effect as an epinephrine or bradykinin antagonist 10. Pizotifen exhibits weak sedative properties in mouse and monkey studies, as indicated by inhibition of locomotion and potentiation of barbiturates, without changes in cardiac or respiratory rates 10. In dogs, intravenous administration of pizotifen cause rapid hypotension but was reversed to normal within 30 minutes 10. Pizotifen was shown to inhibit serotonin uptake in the isolated perfused cat spleen and, in vivo, inhibits serotonin-induced contractions in rat uterus and cat nictiating membrane 2. In contrast, pizotifen demonstrated a venoconstrictor activity in vivo when orally or intravenously administered to saphenous veins in conscious dogs 4. Pizotifen has the potential to stimulate the appetite and may cause weight gain upon treatment 2.
In a double-blind clinical study of patients with mild to moderate depression, treatment of pizotifen led to clinical improvement of the depressive symptoms. However, deterioration of the schizophrenic emotional symptoms was also observed in patients with depression and chronic schizophrenia 1. This indicates that pizotifen may potentially improve the symptoms of patients with depressions in conjunction with migraines 1.
Neuroprotective effect of pizotifen was investigated in vitro in a mouse cell model of Huntington's disease (HD). According to a chemical screen of a mouse HdhQ111/Q111 striatal cell model of HD, treatment of pizotifen was associated with increased ATP levels and decreased activation of caspase-3, leading to enhanced cell viability 6. Transient activation of ERK signalling pathway lasting for less than 3 hours was also observed. In the R6/2 transgenic mouse model of HD, rotarod performance of the mouse treated with pizotifen was seen, accompanied by an increase in DARPP-32 protein expression and restoration of striatal area 6. However these effects being reflected in vivo are not established.
- Mechanism of action
While the mechanism of action is not fully understood, it is proposed that pizotifen works by inhibiting the peripheral actions of serotonin and histamine in increasing the membrane permeability of cranial vessels and transudation of plasmakinin, while altering pain thresholds in migraines 10. By blocking 5-HT receptors, pizotifen attenuates the signalling of serotonin in causing cranial vasoconstriction, as well as serotonin-enhanced platelet function and aggregation 7,9. There is evidence that it also inhibits the peripheral actions of bradykinin 2. Pizotifen may inhibit serotonin reuptake by blood platelets, which affects the tonicity and decreases passive distension of extracranial arteries 10. The effects of pizotifen leading to appetite stimulation may be due to the drug acting at the metabolic level rather than a direct stimulation of the appetite centre 3.
Target Actions Organism UMuscarinic acetylcholine receptor M1 antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans UMuscarinic acetylcholine receptor M3 antagonistHumans U5-hydroxytryptamine receptor 2A antagonistHumans U5-hydroxytryptamine receptor 2B antagonistHumans U5-hydroxytryptamine receptor 2C antagonistHumans U5-hydroxytryptamine receptor 1A partial agonistHumans U5-hydroxytryptamine receptor 1B antagonistHumans UHistamine H1 receptor antagonistHumans UAlpha-1A adrenergic receptor antagonistHumans UAlpha-1B adrenergic receptor antagonistHumans UAlpha-1D adrenergic receptor antagonistHumans UAlpha-2A adrenergic receptor antagonistHumans UAlpha-2B adrenergic receptor antagonistHumans UAlpha-2C adrenergic receptor antagonistHumans - Absorption
The absorption half-life of pizotifen following oral administration is 0.5 to 0.8 hours in an adult male with nearly complete absorption rate of 80%. Maximum blood levels are reached 5 hours post-administration and the absolute bioavailability is 78% 10.
- Volume of distribution
The volume of distribution in an adult male is 833L for pizotifen and 70L for the N-glucuronide conjugate 10.
- Protein binding
Plasma protein binding of pizotifen is > 90% 10.
- Metabolism
Pizotifen is extensively metabolized in the liver, where it primarily undergoes N-glucuronidation to form the main metabolite, N-glucuronide conjugate 10. N-glucuronide conjugate accounts for at least 50% of the plasma and 60-70% of the urinary-excreted radioactivity 10.
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- Route of elimination
About one third of the total orally administered dose is excreted into the feces. Less than 1% of the total dose is excreted in the urine as the unchanged parent drug, and up to 55% of the dose is excreted as its metabolites 10.
- Half-life
The elimination half-life for pizotifen and N-glucuronide conjugate is about 23 hours 10.
- Clearance
Not Available
- Adverse Effects
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The oral Lowest published toxic dose (TDLo) is 12.86 mg/kg in man MSDS. Oral LD50 ranges from 410 to 1500 mg/kg in rat MSDS,10. Oral LD50 in mouse and rabbit is 880 mg/kg and 700 mg/kg, respectively 10. The LD50 following intravenous administration in rat was 17 mg/kg 10.
In adults, the symptoms of overdosage include sedation, drowsiness (preceding excitement, convulsions, and postictal depression), dizziness, hypotension, dryness of the mouth, confusion, tachycardia, ataxia, nausea, vomiting, dyspnea, cyanosis, convulsions, coma, respiratory paralysis and CNS depression 10. Antihistamine toxicity of pizotifen in children may involve excitation, hallucinations, ataxia, incoordination, convulsions, fixed dilated pupils, flushed faces, and fever, leading to coma and cardiorespiratory collapse 10. The use of activated charcoal is recommended in the management of overdose. For drug recent uptake, induction of emesis or gastric lavage and diuresis should be performed 10. Supportive measures should be initiated to maintain effective respiration while closely monitoring vital signs. While severe hypotension must be corrected, the use of adrenaline may produce paradoxical effects 10.
As pizotifen has the potential to cause tachycardia, an ECG should be performed and attention directed at the QRS and QT intervals 10. Excitatory states or convulsions induced by pizotifen may be treated with short-acting barbiturates or benzodiazepines. However analeptics should be avoided 10.
- Pathways
- Not Available
- 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 Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Pizotifen is combined with 1,2-Benzodiazepine. Acebutolol Acebutolol may increase the orthostatic hypotensive activities of Pizotifen. Aceclofenac The risk or severity of hypertension can be increased when Pizotifen is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Pizotifen is combined with Acemetacin. Acenocoumarol The risk or severity of adverse effects can be increased when Pizotifen is combined with Acenocoumarol. - Food Interactions
- Take with or without food. The absorption is unaffected by food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Pizotifen malate 99O99YVR4C 5189-11-7 IWAWCPZVTXCFKD-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sandomigran Tablet 0.50 mg Oral Paladin Labs Inc. 1975-01-01 2021-07-28 Canada 
Sandomigran DS Tablet 1 mg Oral Paladin Labs Inc 1980-12-31 Not applicable Canada
Categories
- ATC Codes
- N02CX01 — Pizotifen
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents producing tachycardia
- Agents that produce hypertension
- Analgesics
- Analgesics, Non-Narcotic
- Anticholinergic Agents
- Antidepressive Agents
- Antimigraine Agents, Miscellaneous
- Antimigraine Preparations
- Central Nervous System Agents
- Central Nervous System Depressants
- Histamine Antagonists
- Histamine H1 Antagonists
- Muscarinic Antagonists
- Nervous System
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Psychotropic Drugs
- Sensory System Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT1 Receptor Antagonists
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Sulfur Compounds
- Thiophenes
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cycloheptathiophenes. These are polycyclic compounds containing a thiophene ring fused to a 7 member carbocyclic moiety. Thiophene is 5-membered ring consisting of four carbon atoms and one sulfur atom.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Cycloheptathiophenes
- Sub Class
- Not Available
- Direct Parent
- Cycloheptathiophenes
- Alternative Parents
- Piperidines / Benzenoids / Thiophenes / Heteroaromatic compounds / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Amine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Cycloheptathiophene / Heteroaromatic compound / Hydrocarbon derivative / Organic nitrogen compound / Organonitrogen compound / Organopnictogen compound
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- benzocycloheptathiophene (CHEBI:50212)
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 0BY8440V3N
- CAS number
- 15574-96-6
- InChI Key
- FIADGNVRKBPQEU-UHFFFAOYSA-N
- InChI
- InChI=1S/C19H21NS/c1-20-11-8-15(9-12-20)19-16-5-3-2-4-14(16)6-7-18-17(19)10-13-21-18/h2-5,10,13H,6-9,11-12H2,1H3
- IUPAC Name
- 1-methyl-4-{6-thiatricyclo[8.4.0.0³,⁷]tetradeca-1(14),3(7),4,10,12-pentaen-2-ylidene}piperidine
- SMILES
- CN1CCC(CC1)=C1C2=C(CCC3=CC=CC=C13)SC=C2
References
- General References
- Standal JE: Pizotifen as an antidepressant. Acta Psychiatr Scand. 1977 Oct;56(4):276-9. [Article]
- Peet KM: Use of pizotifen in severe migraine: a long-term study. Curr Med Res Opin. 1977;5(2):192-9. doi: 10.1185/03007997709110164 . [Article]
- Carroll JD, Maclay WP: Pizotifen (BC 105) in migraine prophylaxis. Curr Med Res Opin. 1975;3(2):68-71. doi: 10.1185/03007997509113649 . [Article]
- Muller-Schweinitzer E: Pizotifen, an antimigraine drug with venoconstrictor activity in vivo. J Cardiovasc Pharmacol. 1986 Jul-Aug;8(4):805-10. [Article]
- Przegalinski E, Baran L, Palider W, Siwanowicz J: The central action of pizotifen. Psychopharmacology (Berl). 1979 Apr 25;62(3):295-300. [Article]
- Sarantos MR, Papanikolaou T, Ellerby LM, Hughes RE: Pizotifen Activates ERK and Provides Neuroprotection in vitro and in vivo in Models of Huntington's Disease. J Huntingtons Dis. 2012;1(2):195-210. doi: 10.3233/JHD-120033. [Article]
- Lin OA, Karim ZA, Vemana HP, Espinosa EV, Khasawneh FT: The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026. doi: 10.1371/journal.pone.0087026. eCollection 2014. [Article]
- Peroutka SJ, Banghart SB, Allen GS: Calcium channel antagonism by pizotifen. J Neurol Neurosurg Psychiatry. 1985 Apr;48(4):381-3. [Article]
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Paladin Labs - Product Monograph: SANDOMIGRAN (Pizotifen hydrogen malate 0.5 mg and 1 mg tablets) [Link]
- External Links
- PubChem Compound
- 27400
- PubChem Substance
- 347827758
- ChemSpider
- 25497
- BindingDB
- 82088
- 8373
- ChEBI
- 50212
- ChEMBL
- CHEMBL294951
- ZINC
- ZINC000000001968
- Wikipedia
- Pizotifen
- MSDS
- Download (340 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral 0.5 mg Tablet Oral 0.50 mg Tablet, coated Oral 0.5 MG Tablet Oral 1 mg Tablet, sugar coated Oral 0.5 mg Syrup 0.25 mg/5ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Partly miscible MSDS - Predicted Properties
Property Value Source Water Solubility 0.00706 mg/mL ALOGPS logP 4.7 ALOGPS logP 4.49 Chemaxon logS -4.6 ALOGPS pKa (Strongest Basic) 7.98 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 1 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 3.24 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 101.1 m3·mol-1 Chemaxon Polarizability 34.36 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-0090000000-b21f77aa98b43b3771f9 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-0090000000-0957d431e75fb4de2199 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-2090000000-1658d01f592e66995fa9 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-0190000000-4236ad739eb7121855e1 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0a4s-2690000000-dbab36317aa3c9a1a734 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-03yr-1190000000-ba972b1a6df02bafc4b4 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]- 175.1331306 predictedDarkChem Lite v0.1.0 [M-H]- 169.58752 predictedDeepCCS 1.0 (2019) [M+H]+ 176.4179306 predictedDarkChem Lite v0.1.0 [M+H]+ 171.94554 predictedDeepCCS 1.0 (2019) [M+Na]+ 175.8776306 predictedDarkChem Lite v0.1.0 [M+Na]+ 178.03868 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- 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
- Eltze M, Mutschler E, Lambrecht G: Affinity profiles of pizotifen, ketotifen and other tricyclic antimuscarinics at muscarinic receptor subtypes M1, M2 and M3. Eur J Pharmacol. 1992 Feb 18;211(3):283-93. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Richards MH: Effects of cyproheptadine and pizotifen on central muscarinic receptors. Eur J Pharmacol. 1991 Apr 3;195(3):403-5. [Article]
- Eltze M, Mutschler E, Lambrecht G: Affinity profiles of pizotifen, ketotifen and other tricyclic antimuscarinics at muscarinic receptor subtypes M1, M2 and M3. Eur J Pharmacol. 1992 Feb 18;211(3):283-93. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Eltze M, Mutschler E, Lambrecht G: Affinity profiles of pizotifen, ketotifen and other tricyclic antimuscarinics at muscarinic receptor subtypes M1, M2 and M3. Eur J Pharmacol. 1992 Feb 18;211(3):283-93. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Przegalinski E, Baran L, Palider W, Siwanowicz J: The central action of pizotifen. Psychopharmacology (Berl). 1979 Apr 25;62(3):295-300. [Article]
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Lin OA, Karim ZA, Vemana HP, Espinosa EV, Khasawneh FT: The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026. doi: 10.1371/journal.pone.0087026. eCollection 2014. [Article]
- Kind
- Protein
- Organism
- Humans
- 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 ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
- Gene Name
- HTR2B
- Uniprot ID
- P41595
- Uniprot Name
- 5-hydroxytryptamine receptor 2B
- Molecular Weight
- 54297.41 Da
References
- Kind
- Protein
- Organism
- Humans
- 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, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51820.705 Da
References
- National Institutes of Health - National Center for Advancing Translational Sciences: Pizotifen Hydrochloride [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- 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...
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- Newman-Tancredi A, Conte C, Chaput C, Verriele L, Audinot-Bouchez V, Lochon S, Lavielle G, Millan MJ: Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy. Naunyn Schmiedebergs Arch Pharmacol. 1997 Jun;355(6):682-8. doi: 10.1007/pl00005000. [Article]
- Kind
- Protein
- Organism
- Humans
- 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 ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
- Gene Name
- HTR1B
- Uniprot ID
- P28222
- Uniprot Name
- 5-hydroxytryptamine receptor 1B
- Molecular Weight
- 43567.535 Da
References
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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) prot...
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Alpha1-adrenergic receptor activity
- Specific Function
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
- Gene Name
- ADRA1D
- Uniprot ID
- P25100
- Uniprot Name
- Alpha-1D adrenergic receptor
- Molecular Weight
- 60462.205 Da
References
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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 oxymetazo...
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 48956.275 Da
References
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Epinephrine 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 clonidine...
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49565.8 Da
References
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Protein homodimerization activity
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- Mylecharane EJ: 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
- Specific Function
- Glucuronosyltransferase activity
- Gene Name
- UGT2B10
- Uniprot ID
- P36537
- Uniprot Name
- UDP-glucuronosyltransferase 2B10
- Molecular Weight
- 60773.485 Da
References
- Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [Article]
Drug created at January 21, 2008 12:21 / Updated at February 20, 2024 23:55