Atomoxetine is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.
 . figure 6.jpg) |
Source | Cephalalgia (2017) . Figure 6. Sumatriptan (Abmole Bioscience, Houston, TX, USA) |
| Method | s.c. with osmotic minipump | |
| Cell Lines | Adult male Sprague-Dawley rats | |
| Concentrations | 0.6 mg/kg/day | |
| Incubation Time | 7 days | |
| Results | Right, but not left, CeA injection of the KOR agonist produced allodynia in sumatriptan-primed rats. |
 . figure 4.jpg) |
Source | Cephalalgia (2017) . Figure 4. Sumatriptan (Abmole Bioscience, Houston, TX, USA) |
| Method | s.c. with osmotic minipump | |
| Cell Lines | Adult male Sprague-Dawley rats | |
| Concentrations | 0.6 mg/kg/day | |
| Incubation Time | 7 days | |
| Results | Nor-BNI administration into the right, but not left, CeA blocked BLS-induced allodynia. |
 . figure 3.jpg) |
Source | Cephalalgia (2017) . Figure 3. Sumatriptan (Abmole Bioscience, Houston, TX, USA) |
| Method | s.c. with osmotic minipump | |
| Cell Lines | Adult male Sprague-Dawley rats | |
| Concentrations | 0.6 mg/kg/day | |
| Incubation Time | 7 days | |
| Results | BLS increases dynorphin content and pKOR expression in the central nucleus of amygdala (CeA). |
 . figure 2.jpg) |
Source | Cephalalgia (2017) . Figure 2. Sumatriptan (Abmole Bioscience, Houston, TX, USA) |
| Method | s.c. with osmotic minipump | |
| Cell Lines | Adult male Sprague-Dawley rats | |
| Concentrations | 0.6 mg/kg/day | |
| Incubation Time | 7 days | |
| Results | Oral CYM51317 administration before BLS prevented cephalic and extracephalic cutaneous allodynia. |
 . figure 1.jpg) |
Source | Cephalalgia (2017) . Figure 1. Sumatriptan (Abmole Bioscience, Houston, TX, USA) |
| Method | s.c. with osmotic minipump | |
| Cell Lines | Adult male Sprague-Dawley rats | |
| Concentrations | 0.6 mg/kg/day | |
| Incubation Time | 7 days | |
| Results | Systemic KOR antagonist nor-BNI prevented stress-induced cephalic and extracephalic allodynia. Systemic KOR antagonist nor-BNI blocked stress-induced increase in plasma CGRP. |
| Molecular Weight | 291.82 |
| Formula | C17H21NO.HCl |
| CAS Number | 82248-59-7 |
| Solubility (25°C) | DMSO 40 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.
[1] Samuele Cortese. Pharmacologic Treatment of Attention Deficit-Hyperactivity Disorder
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