Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H19N5 |
Molecular Weight | 269.3449 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCC1=CNC2=CC=C(CN3C=NC=N3)C=C12
InChI
InChIKey=ULFRLSNUDGIQQP-UHFFFAOYSA-N
InChI=1S/C15H19N5/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3
DescriptionCurator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB00953 | https://www.drugs.com/pro/rizatriptan-orally-disintegrating-tablets.html | http://reference.medscape.com/drug/maxalt-maxalt-mlt-rizatriptan-343033 | https://www.ncbi.nlm.nih.gov/pubmed/9357514
Curator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB00953 | https://www.drugs.com/pro/rizatriptan-orally-disintegrating-tablets.html | http://reference.medscape.com/drug/maxalt-maxalt-mlt-rizatriptan-343033 | https://www.ncbi.nlm.nih.gov/pubmed/9357514
Rizatriptan (trade name Maxalt) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck & Co. for the treatment of migraine headaches. Rizatriptan (trade name Maxalt) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck & Co. for the treatment of migraine headaches. Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors. Rizatriptan binds with high affinity to human cloned 5-HT1B/1D receptors. Rizatriptan benzoate presumably exerts its therapeutic effects in the treatment of a migraine headache by binding to 5-HT1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system. Rizatriptan is completely absorbed following oral administration. The mean oral absolute bioavailability of the rizatriptan benzoate tablet is about 45%, and mean peak plasma concentrations are reached in approximately 1-1.5 hours. The presence of a migraine headache did not appear to affect the absorption or pharmacokinetics of rizatriptan. Food has no significant effect on the bioavailability of rizatriptan but delays the time to reach peak concentration by an hour. The primary route of rizatriptan metabolism is via oxidative deamination by monoamine oxidase-A (MAO-A) to the indole acetic acid metabolite, which is not active at the 5-HT1B/1D receptor. N-mono-desmethyl-rizatriptan, a metabolite with activity similar to that of parent compound at the 5-HT1B/1D receptor, is formed to a minor degree. Plasma concentrations of N-mono-desmethyl-rizatriptan are approximately 14% of those of parent compound, and it is eliminated at a similar rate. Other minor metabolites, the N-oxide, the 6-hydroxy compound, and the sulfate conjugate of the 6-hydroxy metabolite are not active at the 5-HT1B/1D receptor.
CNS Activity
Originator
Sources: http://www.google.com/patents/EP0497512B1
Curator's Comment: # Merck Sharp and Dohme Ltd.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1898 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723 |
10.1 nM [Ki] | ||
Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723 |
3.0 nM [EC50] | ||
Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723 |
140.0 nM [Ki] | ||
Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7752204 |
7.9 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MAXALT Approved UseMAXALT is indicated for the acute treatment of migraine attacks with or without aura in adults. MAXALT is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see CONTRAINDICATIONS). Safety and effectiveness of MAXALT have not been established for cluster headache, which is present in an older, predominantly male population. Launch Date1998 |
|||
Primary | MAXALT Approved UseMAXALT is indicated for the acute treatment of migraine attacks with or without aura in adults. MAXALT is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see CONTRAINDICATIONS). Safety and effectiveness of MAXALT have not been established for cluster headache, which is present in an older, predominantly male population. Launch Date1998 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
44.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
54 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
6.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
12.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
13.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
27.29 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432269/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
28.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
32.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
127 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
16 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
161 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
19 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
33 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
42 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
68 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
69.88 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432269/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
72 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
84 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
97 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
2.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
2.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
2.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
2.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIZATRIPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
10 mg single, oral Recommended |
unhealthy, 17 years n = 1 Health Status: unhealthy Age Group: 17 years Sex: F Population Size: 1 Sources: |
Other AEs: Jaundice... |
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 25 years n = 2 Health Status: unhealthy Age Group: 25 years Sex: M Population Size: 2 Sources: |
Other AEs: Syncope, Incontinence... Other AEs: Syncope (1 patient) Sources: Incontinence (1 patient) |
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 25-29 years n = 2 Health Status: unhealthy Age Group: 25-29 years Sex: M+F Population Size: 2 Sources: |
Other AEs: Dizziness... Other AEs: Dizziness (2 patients) Sources: |
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 29 years n = 2 Health Status: unhealthy Age Group: 29 years Sex: F Population Size: 2 Sources: |
Other AEs: Vomiting, Bradycardia... Other AEs: Vomiting (1 patient) Sources: Bradycardia (1 patient) |
10 mg 2 times / day multiple, oral Recommended Dose: 10 mg, 2 times / day Route: oral Route: multiple Dose: 10 mg, 2 times / day Co-administed with:: tacrolimus(8.5 mg/day; oral) Sources: |
unhealthy, 43 years n = 1 Health Status: unhealthy Age Group: 43 years Sex: M Population Size: 1 Sources: |
Disc. AE: Transient ischemic attack... AEs leading to discontinuation/dose reduction: Transient ischemic attack Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Jaundice | 10 mg single, oral Recommended |
unhealthy, 17 years n = 1 Health Status: unhealthy Age Group: 17 years Sex: F Population Size: 1 Sources: |
|
Incontinence | 1 patient | 80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 25 years n = 2 Health Status: unhealthy Age Group: 25 years Sex: M Population Size: 2 Sources: |
Syncope | 1 patient | 80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 25 years n = 2 Health Status: unhealthy Age Group: 25 years Sex: M Population Size: 2 Sources: |
Dizziness | 2 patients | 80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 25-29 years n = 2 Health Status: unhealthy Age Group: 25-29 years Sex: M+F Population Size: 2 Sources: |
Bradycardia | 1 patient | 80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 29 years n = 2 Health Status: unhealthy Age Group: 29 years Sex: F Population Size: 2 Sources: |
Vomiting | 1 patient | 80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: |
unhealthy, 29 years n = 2 Health Status: unhealthy Age Group: 29 years Sex: F Population Size: 2 Sources: |
Transient ischemic attack | Disc. AE | 10 mg 2 times / day multiple, oral Recommended Dose: 10 mg, 2 times / day Route: oral Route: multiple Dose: 10 mg, 2 times / day Co-administed with:: tacrolimus(8.5 mg/day; oral) Sources: |
unhealthy, 43 years n = 1 Health Status: unhealthy Age Group: 43 years Sex: M Population Size: 1 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Comparative aspects of triptans in treating migraine. | 2001 |
|
Rizatriptan: pharmacological differences from sumatriptan and clinical results. | 2001 |
|
Sumatriptan: pharmacological basis and clinical results. | 2001 |
|
Acute treatment of migraine and the role of triptans. | 2001 Mar |
|
Evidence-based migraine therapy. | 2001 Nov |
|
Cluster headache without autonomic symptoms? | 2001 Nov |
|
Clinical features of withdrawal headache following overuse of triptans and other headache drugs. | 2001 Nov 13 |
|
[Cost effectiveness of treatment with triptanes in Spain]. | 2001 Nov 16-30 |
|
Oral triptans (serotonin 5-HT(1B/1D) agonists) in acute migraine treatment: a meta-analysis of 53 trials. | 2001 Nov 17 |
|
[Therapy of an acute migraine attack. Uniform patient vote for rizatriptan]. | 2001 Nov 22 |
|
Triptans in the treatment of basilar migraine and migraine with prolonged aura. | 2001 Nov-Dec |
|
Advances in pharmacological treatment of migraine. | 2001 Oct |
|
Restoring migraine sufferers' ability to function normally: a comparison of rizatriptan and other triptans in randomized trials. | 2002 |
|
Spotlight on rizatriptan in migraine. | 2002 |
|
Rizatriptan: an update of its use in the management of migraine. | 2002 |
|
Gateways to Clinical Trials. | 2002 Apr |
|
[Satisfaction and recovery of normal activity with rizatriptan 10 mg. Results from the open, prospective, observational 4M study]. | 2002 Dec |
|
Impact of migraine symptoms on health care use and work loss in Canada in patients randomly assigned in a phase III clinical trial. | 2002 Fall |
|
Comparison of triptan tablet consumption per attack: a prospective study of migraineurs in Spain. | 2002 Feb |
|
Migraine: diagnosis, management, and new treatment options. | 2002 Feb |
|
Molecular cloning and expression of the porcine trigeminal ganglion cDNA encoding a 5-ht(1F) receptor. | 2002 Feb 1 |
|
Rizatriptan 5 mg for the acute treatment of migraine in adolescents: a randomized, double-blind, placebo-controlled study. | 2002 Jan |
|
Treatment of migraine with rizatriptan: when to take the medication. | 2002 Jan |
|
Tripstar: a comprehensive patient-based approach to compare triptans. | 2002 Jan |
|
The effect of rizatriptan, ergotamine, and their combination on human peripheral arteries: a double-blind, placebo-controlled, crossover study in normal subjects. | 2002 Jul |
|
Pharmacological treatments for acute migraine: quantitative systematic review. | 2002 Jun |
|
CNS effects of sumatriptan and rizatriptan in healthy female volunteers. | 2002 May |
|
[Controlling migraine with highly effective triptanes. Lowers rate of drug use]. | 2002 May 6 |
|
[Good ruler for assessing effectiveness. Pain free with only one tablet]. | 2002 May 6 |
|
[New meta-analysis of triptanes. Concrete help, so the choice doesn't become overwhelming]. | 2002 May 6 |
|
Sum of Pain Intensity Differences (SPID) in migraine trials. A comment based on four rizatriptan trials. | 2002 Oct |
|
Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials. | 2002 Oct |
|
Comparison of rizatriptan and other triptans on stringent measures of efficacy. | 2002 Sep 10 |
|
Comparison of rizatriptan and other triptans on stringent measures of efficacy. | 2002 Sep 10 |
|
Newer formulations of the triptans: advances in migraine management. | 2003 |
|
Pharmacological approaches to migraine. | 2003 |
|
Crossover comparison of efficacy and preference for rizatriptan 10 mg versus ergotamine/caffeine in migraine. | 2003 |
|
Migraine headache recurrence: relationship to clinical, pharmacological, and pharmacokinetic properties of triptans. | 2003 Apr |
|
[New therapeutic recommendations for severe migraine. High beginning dosage rather than slow dosage increase]. | 2003 Jan 30 |
|
Meta-analysis of oral triptan therapy for migraine: number needed to treat and relative cost to achieve relief within 2 hours. | 2003 Jan-Feb |
|
Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein. | 2003 Jul |
|
Real-world experiences in migraine therapy with rizatriptan. | 2003 Mar |
|
[Highly selective beginning. Associated symptoms and side effects in retrospect]. | 2003 May 26 |
|
An in vitro interethnic comparison of monoamine oxidase activities between Japanese and Caucasian livers using rizatriptan, a serotonin receptor 1B/1D agonist, as a model drug. | 2003 Nov |
|
Rizatriptan RPD for severe migraine in the emergency department--a multicenter study. | 2003 Oct |
|
Naratriptan for the treatment of acute migraine: meta-analysis of randomised controlled trials. | 2004 Feb |
|
Evaluating triptan usage. | 2004 Feb |
|
Defeating migraine pain with triptans: a race against the development of cutaneous allodynia. | 2004 Jan |
|
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons. | 2004 Jan 30 |
|
Fast onset medications through thermally generated aerosols. | 2004 May |
Sample Use Guides
5-10 mg PO at onset of symptoms; repeat dose after 2 hours if necessary; not to exceed 30 mg/24 hr
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9357514
Rizatriptan intrinsic efficacy, expressed as percent of the maximal 5-HT response, was measured in cloned human 5-HT1D and 5-HT1B receptors stably expressed in CHO cells using agonist-induced [35S]GTPγS binding. In this assay, interaction of the agonist-occupied receptor with the G-protein results in dissociation of GDP from the G-protein R-subunit and the binding of a molecule of GTP. Under normal conditions the R-subunit dissociates from the âγ-subunits and, following modulation of its effector, intrinsic R-subunit GTPase hydrolyzes the GTP to GDP. Because [35S]GTPγS is resistant to this GTPase, it accumulates in the membrane and it can be measured by virtue of its radiolabel
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Systematic Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NDF-RT |
N0000175765
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
||
|
NCI_THESAURUS |
C47794
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
||
|
NDF-RT |
N0000175764
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
||
|
WHO-ATC |
N02CC04
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
||
|
NDF-RT |
N0000175763
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
||
|
WHO-VATC |
QN02CC04
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
||
|
LIVERTOX |
857
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
100000080246
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
C61930
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
m9640
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | Merck Index | ||
|
51086HBW8G
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
2393
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
51086HBW8G
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
SUB10346MIG
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
Rizatriptan
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
C093622
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
Rizatriptan
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
CHEMBL905
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
5078
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
DB00953
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
DTXSID2023565
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
48273
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
88014
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | RxNorm | ||
|
51
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
144034-80-0
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY | |||
|
7474
Created by
admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE (PARENT)
METABOLITE (PARENT)
METABOLITE (PARENT)
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)