生物活性 Pardoprunox (SLV-308) hydrochloride is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively[1].
体外研究 (In Vitro) Pardoprunox (SLV-308) hydrochloride acts as a potent but partial D2 receptor agonist (pEC50= 8.0 and pA2=8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox hydrochloride acts as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC50=9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA2=9.0). Pardoprunox hydrochloride acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50=6.3)[1].
分子量 269.73
性状 Solid
Formula C12H16ClN3O2
CAS 号 269718-83-4
中文名称 盐酸帕多芦诺
运输条件 Room temperature in continental US; may vary elsewhere.
溶解性数据 In Vitro: DMSO : 150 mg/mL (556.11 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
配制储备液 浓度溶剂体积质量 1 mg 5 mg 10 mg 1 mM 3.7074 mL 18.5371 mL 37.0741 mL 5 mM 0.7415 mL 3.7074 mL 7.4148 mL 10 mM 0.3707 mL 1.8537 mL 3.7074 mL * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: