产品介绍 |
Medetomidine 是一种具有口服活性的 α2 肾上腺素受体 (α2-adrenoceptor) 激动剂 (Ki: 1.08 nM)。Medetomidine 具有镇静和镇痛作用。Medetomidine 可通过激活血管上的 α2 肾上腺素能受体引起外周血管收缩。
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生物活性 |
Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels[4].
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体外研究 |
Medetomidine (0-1 µM, 1 h) inhibits aldosterone release from the adrenocortical cell suspension[7].
Medetomidine (10 nM) activates a kicking response in Cyprids[8].
Medetomidine (1 µM) increases cellular cAMP production by activating β-like receptors in CHO cells[8].
西域 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 |
Medetomidine (200 μg/kg, p.o. or i.m.) induces a sedation in cats[4].
Medetomidine (20 µg/kg, i.v.) shows sedative and analgesic effects in dogs[5].
Medetomidine (0.05-0.3 mg/kg, s.c.) protects against Diazinon-induced toxicosis in mice[6].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Diazinon (75 mg/kg, orally)-induced toxicosis in mice[6] |
Dosage: |
0.05, 0.1 and 0.3 mg/kg |
Administration: |
Subcutaneous injection (s.c.), 15 min before Diazinon. |
Result: |
Protected the mice from the toxicity induced by Diazinon.
Decreased the occurrence of Straub tail, excessive salivation and tremor.
Increased the latencies to onset of tremor and death when compared with control.
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Animal Model: |
Dogs[5] |
Dosage: |
20 µg/kg |
Administration: |
Intravenous injection (i.v.) |
Result: |
Showed sedative and analgesic effects.
Increased in SAP, MAP, DAP, MPAP, PCWP, CVP, SVR, PVR, core body temperature.
Decreased in HR, CO, CI, SV, SI, RR, pH.
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体内研究 |
Medetomidine (200 μg/kg, p.o. or i.m.) induces a sedation in cats[4].
Medetomidine (20 µg/kg, i.v.) shows sedative and analgesic effects in dogs[5].
Medetomidine (0.05-0.3 mg/kg, s.c.) protects against Diazinon-induced toxicosis in mice[6].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Diazinon (75 mg/kg, orally)-induced toxicosis in mice[6] |
Dosage: |
0.05, 0.1 and 0.3 mg/kg |
Administration: |
Subcutaneous injection (s.c.), 15 min before Diazinon. |
Result: |
Protected the mice from the toxicity induced by Diazinon.
Decreased the occurrence of Straub tail, excessive salivation and tremor.
Increased the latencies to onset of tremor and death when compared with control.
|
Animal Model: |
Dogs[5] |
Dosage: |
20 µg/kg |
Administration: |
Intravenous injection (i.v.) |
Result: |
Showed sedative and analgesic effects.
Increased in SAP, MAP, DAP, MPAP, PCWP, CVP, SVR, PVR, core body temperature.
Decreased in HR, CO, CI, SV, SI, RR, pH.
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性状 | Solid |
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溶解性数据 |
In Vitro:
DMSO : 250 mg/mL (1248.25 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
配制储备液
浓度
溶剂体积
质量
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1 mg |
5 mg |
10 mg |
1 mM |
4.9930 mL |
24.9650 mL |
49.9301 mL |
5 mM |
0.9986 mL |
4.9930 mL |
9.9860 mL |
10 mM |
0.4993 mL |
2.4965 mL |
4.9930 mL |
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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。-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:
——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: ≥ 2.5 mg/mL (12.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.48 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 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。
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2.
请依序添加每种溶剂: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.48 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。
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3.
请依序添加每种溶剂: 10% DMSO 90% corn oil Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.48 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 25.0 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 西域 网站选购。
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Powder |
-20°C |
3 years |
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4°C |
2 years |
In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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参考文献 |
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. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[Content Brief]
. Kallio A, et al. Acute effects of medetomidine, a selective alpha 2-adrenoceptor agonist, on anterior pituitary hormone and cortisol secretion in man. Acta Endocrinol (Copenh). 1988 Sep;119(1):11-5.
[Content Brief]
. R Virtanen, et al. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist.
[Content Brief]
[4]. O. B. Ansah, et al. Comparing oral and intramuscular administration of medetomidine in cats.
[5]. Kuo WC, et al. Comparative cardiovascular, analgesic, and sedative effects of medetomidine, medetomidine-hydromorphone, and medetomidine-butorphanol in dogs. Am J Vet Res. 2004 Jul;65(7):931-7.
[Content Brief]
[6]. Yakoub LK, et al. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8.
[Content Brief]
[7]. Jager LP, et al. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6.
[Content Brief]
[8]. Ulrika Lind, et al. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine.
[Content Brief]
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