Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.48%
产品类别：
抑制剂
货号：
T7519
Product Introduction
Bioactivity
名称
RS-127445 hydrochloride
描述
RS-127445 hydrochloride (MT 500) is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist(pKi : 9.5).
动物实验
Rats were euthanized.?Right and left external jugular veins were dissected, cleaned of connective tissues and cut into ring segments approximately 5 mm long.?Tungsten hooks (0.125 mm diameter) were inserted through the lumen of the vein and connected to tension transducers.?Tissues were kept in 10 ml organ baths containing Kreb's solution supplemented with cocaine (30 μm), corticosterone (30 μm), ketanserin (0.3 μm) and indomethacin (3 μm) at 37°C at a resting tension of 0.5 g.?Prior to the initiation of any studies, monamine oxidases were inactivated by a 30 min pre exposure of the tissue to pargyline (0.1 mm).?The veins were then exposed to 0.1 μm U46619 (9,11-dideoxy-9 α, 11 aα-methano-epoxy-PGF2α;?a thromboxane A2 mimetic) until a stable contraction was attained.?Acetylcholine (0.1 μm) was used to verify the integrity of the endothelium and to determine the maximum amount of nitric?oxide-dependent relaxation that was achievable.?After washout of the acetylcholine and recontraction with U46619, cumulative concentration-response curves to (±)-α-methyl-5-HT were constructed.?When maximum relaxation was reached, the baths were rinsed, and the tissues were maintained undisturbed for 2 h. Antagonists (RS 127445)were then added to the bath and allowed to equilibrate with the tissue for at least 1 h before a second concentration-response curve to (±)-α-methyl-5-HT was generated[1].
