FK962 is an enhancer of somatostatin release, exerts cognitive-enhancing actions. FK962 significantly reduces somatostatin-induced inhibition of Ca2+ channels at 1-100 nM in single rat hippocampal neurons using whole-cell patch-clamp. FK962 (1 nM-1 μM) also significantly enhances high K+-evoked somatostatin release from rat hippocampal slices.
In vivo, FK962 (0.1, 0.3 or 1.0 mg/kg; i.p.) and Donepezil (a single dose of 1 mg/kg) act synergistically to improve cognition in rats.
| Molecular Weight | 264.3 |
| Formula | C14H17FN2O2 |
| CAS Number | 283167-06-6 |
| 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.
| Related Somatostatin Receptor Products |
|---|
| TT-232
TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. |
| Cyclosomatostatin
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. |
| Somatostatin-28 (1-14)
Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28. |
| CH 275
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. |
| CYN 154806
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist. |
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