Ro60-0175 是一种有效的选择性5-HT2C受体激动剂。Ro60-0175 降低了可卡因的成瘾性以及可卡因在戒断反应消失后重新成瘾的可能性。
生物活性 | Ro60-0175 is a potent and selective agonist of5-HT2Creceptor. Ro60-0175 reduces cocaine self-administration, and the ability of cocaine to reinstate responding after extinction of drug-seeking behavior[1]. |
IC50& Target | |
体内研究 (In Vivo) | Ro60-0175 (1 mg/kg; s.c.) preserves the regularity of responding seen in control animals in drug-treated group, but drug-treated animals reach their break-points earlier[1]. Ro60-0175 (0.5 mg/kg (SB242084); 1 mg/kg (Ro60-0175); s.c., i.p.) reduces responding for cocaine and effect is reversed by SB242084[1]. Ro60-0175 (0.3, 1, and 3 mg/kg (Ro60-0175); 1 mg/kg (yohimbine); s.c.; i.p.) dose dependently attenuates the response increased by the yohimbine treatment alone relative to vehicle injection[1]. Ro60-0175 (0.5 mg/kg (SB242084); 1 mg/kg (Ro60-0175); 1 mg/kg (yohimbine); s.c.; i.p.) reduces responding and that this effect is prevented by SB242084 pretreatment[1]. Ro60-0175 (0.3, 1, and 3 mg/kg; s.c.) significantly reduces responding on the active lever in the reinstatement group[1]. Ro60-0175 (0.5 mg/kg SB242084; 1 mg/kg Ro60-0175; s.c.; i.p.) reduces responding compared to vehicle in the reinstatement group, and that this effect is prevented by pretreatment with SB242084. For responding on the inactive lever, there are no significant main effects or interactions[1].
Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | Dosage: | 1 mg/kg | Administration: | s.c. | Result: | Preserved the regularity of responding seen in control animals in drug-treated group, but drug-treated animals reached their break-points earlier. |
Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | Dosage: | 0.5 mg/kg (SB242084), 1 mg/kg (Ro60-0175) | Administration: | s.c. (Ro60-0175), i.p. (SB242084) | Result: | Reduced responding for cocaine and effect was reversed by SB242084. |
Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | Dosage: | 0.3, 1, and 3 mg/kg (Ro60-0175), 1 mg/kg (yohimbine) | Administration: | s.c. (Ro60-0175), i.p. (yohimbine) | Result: | Showed yohimbine treatment alone increased responding relative to vehicle injection, and the response was attenuated dose dependently by Ro60-0175. |
Animal Model: | Adult male Sprague-Dawley rats (280-320 g)[1] | Dosage: | 0.5 mg/kg (SB242084), 1 mg/kg (Ro60-0175), 1 mg/kg (yohimbine) | Administration: | s.c. (Ro60-0175), i.p. (yohimbine), i.p. (SB242084) | Result: | Ro60-0175 reduced responding and that this effect was prevented by SB242084 pretreatment. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 125 mg/mL(551.44 mM;Need ultrasonic) 配制储备液 1 mM | 4.4115 mL | 22.0575 mL | 44.1151 mL | 5 mM | 0.8823 mL | 4.4115 mL | 8.8230 mL | 10 mM | 0.4412 mL | 2.2058 mL | 4.4115 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (9.18 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.18 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (9.18 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.18 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (9.18 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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