RO-5328673

• Target:

  Others

• Related Pathways:

  Others

• Bioactivity:

  RO-5328673 is a dual NK2/NK3 antagonist. O5328673. [ (3) H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [ (3) H]IP accumulation assay. In binding kinetic analyses, [ (3) H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of gp SNpc, RO5328673 inhibited the senktide-induced potentiation of spontaneous activity of dopaminergic neurons with an insurmountable mechanism of action. RO5328673 exhibited in-vivo activity in gerbils, robustly reversing the senktide-induced locomotor activity.

• Smiles:

  N (C (OC1=CC=C (F) C=C1) =O) (C) [C@H]2[C@@H] (CN (C (=O) C3CCN (C (=O) C4 (C) CC4) CC3) C2) C5=CC (Cl) =C (Cl) C=C5

• Molecular Formula:

  C29H32Cl2FN3O4

• Molecular Weight:

  576.49

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  1310817-94-7