Nizatidine?is a histamine H2-receptor antagonist with and IC50 of 6.7 nM for AChE. It inhibits stomach acid production, and commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD). The relative anti-AChE potency was in the following order: neostigmine > nizatidine >cimetidine >> famotidine. The inhibition of AChE by nizatidine was noncompetitive, with a Ki value of 7.4 x 10 nM. Gastrointestinal (GI) motility was examined during the interdigestive state in dogs with chronically implanted force transducers.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Rat |
| Formulation | saline |
| Dosages | 0.5-10 μmol/kg |
| Administration | s.c |
| Molecular Weight | 331.46 |
| Formula | C12H21N5O2S2 |
| CAS Number | 76963-41-2 |
| Solubility (25°C) | DMSO 60 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.
[2] No authors listed. Nizatidine
[3] No authors listed. Nizatidine
[4] J T Callaghan, et al. A pharmacokinetic profile of nizatidine in man
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