Yangambin

Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC₅₀ of 29.7 μM and a K_i of 17.1 μM against human UGT1A1, and an IC₅₀ of 56.5 μM and a K_i of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB₄-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca²⁺ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases^{[1][2][3][4][5][6]}. IC50 & Target:PAF, Ca²⁺ channels^[1] In Vitro:Yangambin (50-200 μM; 48 h) potently reduces the viability and survival rate of Leishmania amazonensis in bone marrow-derived macrophages from BALB/c mice, with IC₅₀ values of 43.9 μM and 76 μM, respectively^[3].
Yangambin (100 μM; 48 h) reduces the production of NO, TNF-α, IL-6 and PGE₂, and increases the production of IL-10, in bone marrow-derived macrophages from BALB/c mice infected with Leishmania amazonensis and stimulated with IFN-γ^[3].
Yangambin (0.1 μM-1 mM; pre-incubated prior to 60 mM K⁺Cl⁻ stimulation) inhibits K⁺Cl⁻-induced intracellular calcium signals in Fura-2/AM (HY-101897)-loaded rat mesenteric artery smooth muscle cells in a concentration-dependent manner, with significant inhibitory effects observed at concentrations of 30 μM and 1 mM^[5].
Yangambin (0.1-200 µM; 60 min) inhibits the activities of UGT1A1 and UGT1A3 in pooled human liver microsomes, with IC₅₀ values of 29.7 µM and 56.5 µM, respectively^[6].
Yangambin (2-40 µM; 30 min) non-competitively inhibits UGT1A1-catalyzed glucuronidation of SN-38 in pooled human liver microsomes, with a K_i value of 17.1 µM^[6].
Yangambin (5-80 µM; 30 min) competitively inhibits UGT1A3-catalyzed 24-acyl glucuronidation of chenodeoxycholic acid in pooled human liver microsomes, with a K_i value of 66.8 µM^[6]. In Vivo:Yangambin (10-20 mg/kg; i.p.; single administration 1 hour prior to challenge) significantly inhibits antigen-induced pleural neutrophil and eosinophil infiltration in sensitized rats, but exerts no inhibitory effect on exudation, and suppresses thrombocytopenia^[1].
Yangambin (10-20 mg/kg; i.p.; single administration 1 hour prior to challenge) significantly inhibits platelet-activating factor (PAF)-induced pleural eosinophil accumulation in normal rats. At the dose of 20 mg/kg, it inhibits PAF-induced neutrophil infiltration, but has no effect on exudation, partially inhibits hemoconcentration and leukocytosis, and almost completely blocks thrombocytopenia^[1].
Yangambin (20 mg/kg; i.p.; single administration 1 hour prior to challenge) significantly inhibits LTB₄ (HY-107608)-induced pleural neutrophil infiltration in normal rats^[1].
Yangambin (12.5-50 mg/kg; i.p.; single administration) exerts central nervous system depressant activity in healthy male Swiss mice, reduces spontaneous and upright locomotor activities, prolongs immobility time in the forced swimming test, and alters parameters of the elevated plus maze; it also shortens pentobarbital sleep latency and prolongs pentobarbital-induced sleep duration^[2].
Yangambin (10-20 mg/kg; i.v.; single bolus) dose-dependently and selectively inhibits PAF-induced cardiovascular changes and thrombocytopenia in anesthetized rabbits^[4].
Yangambin (1-30 mg/kg; i.v.) induces dose-dependent hypotension and tachycardia in normotensive, unanesthetized male Wistar rats^[5].