Levocabastine hydrochloride

Levocabastine hydrochloride is a potent, selective histamine H1 receptor antagonist and a high-affinity neuropeptide V receptor subtype 2 (NTR2) antagonist (Ki = 17 nM). In addition, it exhibits VLA-4 antagonistic activity and can inhibit eosinophil infiltration in allergic conjunctivitis.

NTR2:17 nM (Ki)

Method: Human Jurkat cells were treated with Levocabastine hydrochloride (100 and 400 μM) for 30 min, and flow cytometry (FACS) was used to assess its competitive binding with anti-α4 integrin antibody.
Result: Levocabastine hydrochloride (100 and 400 μM) concentration-dependently inhibited the binding of anti-α4 integrin antibody to α4 integrin on the surface of Jurkat cells ^[2].

Method: Mice were subjected to acute restraint stress, then administered β-LT (30 mg/kg) intraperitoneally, followed 10 min later by intraperitoneal injection of Levocabastine hydrochloride (0.05 mg/kg). The hole-board test was used to assess the hole-poking behavior of the mice.
Result: Levocabastine hydrochloride significantly blocked the anti-stress effect of β-LT, which increased the number of hole-pokes in restraint-stressed mice, reducing the hole-poke count from 25.78 ± 1.59 to 17.67 ± 1.01. In terms of hole-poke latency, Levocabastine hydrochloride showed a tendency to block the latency-shortening effect of β-LT ^[1].

DMSO: Soluble