Dihydroergotamine mesylate is an ergot alkaloid used to treat migraines. Target: 5-HT Receptors Dihydroergotamine is not as effective as sumatriptan or phenothiazines as a single agent for treatment of acute migraine headache; however, when administered with an antiemetic, dihydroergotamine appears to be as effective as opiates, ketorolac, or valproate. Given its nonnarcotic properties, parenteral dihydroergotamine combined with an antiemetic should be considered as effective initial therapy in clinical practice. The introduction of the intranasal formulation of DHE provides both pharmacologic and patient-convenience advantages for use in migraine therapy [2, 3].
Molecular Weight | 679.78 |
CAS Number | 6190-39-2 |
Solubility (25°C) | DMSO 50 mg/mL |
Storage | 2-8°C, protect from light, dry, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] R B Lipton. Headache. Ergotamine tartrate and dihydroergotamine mesylate: safety profiles
Related 5-HT Receptor Products |
---|
Vabicaserin hydrochloride
Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM. |
TC-2153
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP). TC-2153 also inhibits 5-HT2A receptor-mediated signaling. |
Gentisein
Gentisein (NSC-329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM. |
MM120
MM120 is a synthetic tryptamine that is also a partial agonist at the 5-hydroxytryptamine 2A (5-HT2A) receptor. It can be used in studies related to GAD and attention deficit hyperactivity disorder (ADHD). |
SB 258741 hydrochloride
SB 258741 hydrochloride is a specific 5-HT7 receptor antagonist for schizophrenia. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.