AD258 is a Sigma Receptor Ligand with Potent Antiallodynic Activity. AD258 exhibited negligible in vitro cellular toxicity and a high binding affinity to both SRs (KiS1R = 3.5 nM, KiS2R = 2.6 nM), but not for other pain-related targets, and exerted high potency in a model of capsaicininduced allodynia, reaching the maximum antiallodynic effect at very low doses (0.6−1.25 mg/kg). Functional activity experiments showed that S1R antagonism is needed for the effects of AD258 and that it did not induce motor impairment. In addition, AD258 exhibited a favorable pharmacokinetic profile.
MedKoo Cat#: 124618
Name: AD258
CAS#: N/A
Chemical Formula: C22H25N3
Exact Mass: 331.2000
Molecular Weight: 331.46
Elemental Analysis: C, 79.72; H, 7.60; N, 12.68
The following data is based on the product molecular weight 331.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
