Eltoprazine hyrochloride is a serotonin 5-HT1A/1B receptor agonist that has been shown to reduce L-DOPA-induced dyskinesias in in experimental models of Parkinson′s Disease and in human patients. It has Ki values for 5-HT1A, 5-HT1B and 5-HT1C receptors of 40 nM and 52 nM, respectively.
| Molecular Weight | 256.73 |
| Formula | C12H16N2O2 · HCl |
| CAS Number | 98206-09-8 |
| Form | Solid |
| Solubility (25°C) | Water: 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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] Sharon B Wigal, et al. Pharmacokinetic evaluation of eltoprazine
[5] B Olivier, et al. Behavioural pharmacology of the serenic, eltoprazine
| 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.
