| Chemical Properties | Back Directory | [Boiling point ]
678.370±55.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.210±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
4.386±0.10(predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases[1]. | [in vivo]
HY-078020 (5 mg/kg, i.g.) inhibits the histamine induced skin vasodilation and capillary permeability in ICR/KM mice, with a vascular permeability inhibition rates of 58.71 %[1].
HY-078020 (10 mg/kg, i.v.) exhibits aweak anticholinergic activity with an inhibition rate of salivary secretion of 10.8% in Wistar mice[1].
HY-078020 reveals a pharmacokinetic profils in mice[1]:
Pharmacokinetic Analysis of HY-078020 in wistar male rats[1]
| route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (ng·h/mL) | AUC0-inf (ng·h/mL) | Vd (L/kg) | CL (mL/h/kg) | MRT0-inf(h) | F (%) | | iv | 4 | 0.653 ± 0.12 | - | - | 1678 ± 152.59 | 1822.38 ± 224.97 | 1.77 ± 0.22 | 37.00 ± 4.62 | 0.70 ± 0.14 | 59.55 | | po | 25 | 4.05 ± 0.81 | 0.38 ± 0.16 | 1722.06 ± 337.11 | 6246.92 ± 1443.28 | 7209.70 ± 1419.01 | 21.26 ± 7.42 | 59.35 ± 10.59 | 6.01 ± 1.42 | - |
| Animal Model: | histamine-induced vascular permeability in ICR and Kunming mice[1] | | Dosage: | 5 mg/kg | | Administration: | i.g. | | Result: | Reduced the vascular permeability with an inhibition rate of 58.71%. |
| Animal Model: | Wistar mice[1] | | Dosage: | 10 mg/kg | | Administration: | i.v., once a day | | Result: | Inhibited salivary secretion with an inhibition rate of 10.8%. |
| [IC 50]
H1 Receptor: 24.12 nM (IC50); mAChR3 | [References]
[1] Chu Z, et al., Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases. Eur J Med Chem. 2024 Feb 3;268:116197. DOI:10.1016/j.ejmech.2024.116197 |
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