Levocabastine (R 50547) hydrochloride 是一种强效选择性组胺 H1 受体拮抗剂。Levocabastine hydrochloride 也是一种选择性、高亲和力的神经降压素受体亚型 2(NTR2)拮抗剂，对 mNTR2 的Ki值为 17 nM。Levocabastine hydrochloride 可作为VLA-4拮抗剂，干扰过敏性结膜炎 (AC) 结膜嗜酸性粒细胞的浸润。
| 生物活性 | Levocabastine (R 50547) hydrochloride is a potent and selectivehistamine H1-receptorantagonist. Levocabastine hydrochloride is also a selective, high affinityneurotensin receptorsubtype 2 (NTR2)antagonist, with aKiof 17 nM for mNTR2. Levocabastine hydrochloride can act as aVLA-4antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3]. |
| IC50& Target[1] | H1Receptor | NTR2 17 nM (Ki) |
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体外研究
(In Vitro) | Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of125I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC50of 406.2μm[3].
Levocabastine (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells) hydrochloride inhibits α4β1 integrin/VCAM-1-mediated cell adhesion in vitro. Levocabastine inhibits α4β1 integrindependent adhesion of Jurkat cells to VCAM-1 with an IC50of 395.6 μM, and the adhesion of EoL-1 cells with an IC50of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC50=443.7 μM)[3].
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体内研究
(In Vivo) | Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) hydrochloride inhibits the virus-induced airway hyperresponsiveness[1].
Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) hydrochloride blocks anti-stress effect ofβ-LT on mouse behavior[2].
Levocabastine (500 μg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) hydrochloride induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4[3].
| Animal Model: | Guinea-pig with Parainfluenza-3 (PI-3) virus[1] | | Dosage: | 0.25 mg/kg | | Administration: | Intraperitoneal injection; twice a day for five days | | Result: | Suppressed the influx of broncho-alveolar cells and increased in albumin content. |
| Animal Model: | Male C57BL/6J mice (8-9 weeks old)[2] | | Dosage: | 0.05 mg/kg; 30 mg/kg (β-LT) | | Administration: | Intraperitoneal injection; once | | Result: | Blocked the anxiolytic effect ofβ-LT and decreased the number of head-dips. |
| Animal Model: | Ovalbumin-sensitized guinea pigs[3] | | Dosage: | 500 μg/eye | | Administration: | drops eye, once | | Result: | Produced a noteworthy protection from allergic conjunctivitis (AC) and prevented the conjuctival elevation of VLA-4 as well as conjunctival eosinophil infiltration. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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