GSK172981 is a non-peptide tachykinin NK3 receptor antagonist. GSK172981 demonstrated high affinity for recombinant human (pK(i) value 7.7) and native guinea pig (pK(i) value 7.8) tachykinin NK(3) receptors. In vitro functional evaluations revealed GSK172981 to be a competitive antagonist (pA(2)=7.2) at cloned human tachykinin NK(3) receptor. GSK172981 also exhibited a competitive profile in antagonizing neurokinin B-stimulated neuronal activity recorded from the guinea pig medial habenula slices (apparent pK(B)=8.1). GSK172981 is potentially useful in the treatment of schizophrenia.
MedKoo Cat#: 526725
Name: GSK172981
CAS#: 1133705-99-3
Chemical Formula: C26H22FN3O
Exact Mass: 411.1747
Molecular Weight: 411.48
Elemental Analysis: C, 75.89; H, 5.39; F, 4.62; N, 10.21; O, 3.89
The following data is based on the product molecular weight 411.48 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 |
