Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H19N5 |
Molecular Weight | 269.3454 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCc1c[nH]c2ccc(cc12)Cn3cncn3
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
Molecular Formula | C15H19N5 |
Molecular Weight | 269.3454 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 Date8.9907842E11 |
|||
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 Date8.9907842E11 |
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 |
---|---|---|
A comparison of visual analog scale and categorical ratings of headache pain in a randomized controlled clinical trial with migraine patients. | 2001 Aug |
|
Rizatriptan wafer--sublingual vs. placebo at the onset of acute migraine. | 2001 Feb |
|
Safety and rational use of the triptans. | 2001 Jul |
|
Influence of beta-adrenoceptor antagonists on the pharmacokinetics of rizatriptan, a 5-HT1B/1D agonist: differential effects of propranolol, nadolol and metoprolol. | 2001 Jul |
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Acute treatment of migraine and the role of triptans. | 2001 Mar |
|
Meta-analysis of rizatriptan efficacy in randomized controlled clinical trials. | 2001 Mar |
|
Efficacy and tolerability of rizatriptan 10 mg in migraine: experience with 70 527 patient episodes. | 2001 Mar |
|
Evidence-based migraine therapy. | 2001 Nov |
|
[Therapy of an acute migraine attack. Uniform patient vote for rizatriptan]. | 2001 Nov 22 |
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Advances in pharmacological treatment of migraine. | 2001 Oct |
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Comparison of rizatriptan and other triptans on stringent measures of efficacy. | 2001 Oct 23 |
|
What matters is not the differences between triptans, but the differences between patients. | 2001 Sep |
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Rizatriptan: an update of its use in the management of migraine. | 2002 |
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[Satisfaction and recovery of normal activity with rizatriptan 10 mg. Results from the open, prospective, observational 4M study]. | 2002 Dec |
|
Migraine: diagnosis, management, and new treatment options. | 2002 Feb |
|
Rizatriptan 5 mg for the acute treatment of migraine in adolescents: a randomized, double-blind, placebo-controlled study. | 2002 Jan |
|
[Treatment of migraine in patients with hypertension and ischemic heart disease]. | 2002 Jan 20 |
|
Gateways to Clinical Trials. June 2002. | 2002 Jun |
|
Rizatriptan combined with rofecoxib vs. rizatriptan for the acute treatment of migraine: an open label pilot study. | 2002 May |
|
Determinants of migraine-specific quality of life. | 2002 Oct |
|
Sum of Pain Intensity Differences (SPID) in migraine trials. A comment based on four rizatriptan trials. | 2002 Oct |
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Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials. | 2002 Oct |
|
Newer formulations of the triptans: advances in migraine management. | 2003 |
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Crossover comparison of efficacy and preference for rizatriptan 10 mg versus ergotamine/caffeine in migraine. | 2003 |
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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 |
|
[Highly selective beginning. Associated symptoms and side effects in retrospect]. | 2003 May 26 |
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Cost-effectiveness of almotriptan and rizatriptan in the treatment of acute migraine. | 2003 Nov |
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Patient-reported benefits of rizatriptan compared with usual non-triptan therapy for migraine in a primary care setting. | 2003 Nov |
|
Triptans for treatment of acute pediatric migraine: a systematic literature review. | 2003 Nov |
|
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 |
|
[It impairs quality of life and work time. Migraine therapy should not be left to the patients!]. | 2003 Nov 27 |
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Endothelium-dependent relaxant responses to selective 5-HT(1B/1D) receptor agonists in the isolated middle cerebral artery of the rat. | 2003 Nov-Dec |
|
Rizatriptan RPD for severe migraine in the emergency department--a multicenter study. | 2003 Oct |
|
Investigation of the effects of naratriptan, rizatriptan, and sumatriptan on jugular venous oxygen saturation in anesthetized pigs: implications for their mechanism of acute antimigraine action. | 2003 Oct |
|
Migraine: diagnosis and management. | 2003 Sep-Oct |
|
Naratriptan for the treatment of acute migraine: meta-analysis of randomised controlled trials. | 2004 Feb |
|
Evaluating triptan usage. | 2004 Feb |
|
Productivity cost benefit to employers of treating migraine with rizatriptan: a specific worksite analysis and model. | 2004 Jan |
|
Defeating migraine pain with triptans: a race against the development of cutaneous allodynia. | 2004 Jan |
|
CNS effects of sumatriptan and rizatriptan. | 2004 Jan |
|
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Jun 26 02:22:58 UTC 2021
by
admin
on
Sat Jun 26 02:22:58 UTC 2021
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Record UNII |
51086HBW8G
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000175765
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NCI_THESAURUS |
C47794
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NDF-RT |
N0000175764
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WHO-ATC |
N02CC04
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NDF-RT |
N0000175763
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WHO-VATC |
QN02CC04
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LIVERTOX |
857
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C61930
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M9640
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PRIMARY | Merck Index | ||
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51086HBW8G
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2393
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SUB10346MIG
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Rizatriptan
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C093622
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Rizatriptan
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CHEMBL905
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5078
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DB00953
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144034-80-0
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88014
Created by
admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
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PRIMARY | RxNorm | ||
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51
Created by
admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
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PRIMARY | |||
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144034-80-0
Created by
admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
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PRIMARY | |||
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7474
Created by
admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
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PRIMARY |
Related Record | Type | Details | ||
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EXCRETED UNCHANGED |
Approximately 26 and 14% of i.v. and oral rizatriptan doses, respectively, were excreted in urine as intact parent drug
URINE
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SALT/SOLVATE -> PARENT | |||
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TARGET -> AGONIST | |||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> AGONIST |
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
The mono N-desmethyl metabolite has intrinsic potency that is about 3-fold lower. Its contribution to in vivo efficacy is probably very low or negligible, since circulating concentrations are about one-tenth those of the parent drug
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METABOLITE -> PARENT |
after i.v. (3-mg)
URINE
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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