Antibodies
Medetomidine HCl
- 貨號 Cat. No.
- S3060
- 規格 Size
- 10mM/1mL~50mg
- 品牌 Brand
- Selleckchem
Description
Medetomidine HCl
Catalog No.S3060
Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
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Biological Activity
| Description | Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor. | |||||
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| Targets | α2-adrenoceptor | |||||
| IC50 | 1.08 nM (Ki ) [1] | |||||
| In vitro | Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has very weak or no binding to other neurotransmitter receptors. [1] | |||||
| In vivo | In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a dose-dependent, relatively short-lived reduction in blood pressure and heart rate. In the pithed rat, medetomidine shows very potent vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg) effects without affecting basal heart rate. [2] Medetomidine induces dose-dependent sedation, which at high doses (>100μg/kg) includes loss of the righting reflex and hypothermia. Medetomidine induces a decreases in the turnover rate of biogenic amines in the brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits brain dopamine turnover at high doses, decreases serotonin turnover. [3] | |||||
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Protocol(Only for Reference)
Kinase Assay: [1]
| Receptor binding experiments | Rats are killed and the brains are immediately removed from the skulls, dissected free of the cerebella and homogenized in ice-cold Tris-HC1 buffer. The homogenate is then centrifuged for 5 min at 500 × g at 4 °C and the supernatant fraction is further centrifuged two times at 50,000 × g for 20 min (4 °C), with re-homogenization of the pellet with 20 volumes of fresh buffer followed by centrifugation. The washed pellet is suspensed in Tris-HC1 buffer at approximately 1 and 4 mg protein/ml for [3H]prazosin and [3H]clonidine binding assays, respectively. Binding reaction mixtures contains (in a final volume of 0.5 ml): 50 mM Tris-HC1 (pH 7.7 for [3H]prazosin and pH 7.5 for [3H]clonidine binding assay, respectively), [3H]prazosin 0.5 nM or [3H]clonidine 4 nM, membrane suspension (0.1 ml), ligand to be tested (0.01-0.2 ml) or phentolamine (10 μM) for determination of non-specific binding. MgC12 (10 mM) is also added to the mixture in the [3H]clonidine binding studies. The incubations are performed in triplicate at 25°C for 30 min and are stopped by rapid filtration under suction through Whatman GF/B glass fibre filters followed by three rinses with 5 ml ice-cold buffer. The filters are dried and solubilized in Instagel for 18 h. Radioactivity is counted in a Wallacliquid scintillation counter equipped with external standard and a built-in computer for d.p.m. (disintegration per min) calculation, with reference to standard quench curves for tritium. |
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Animal Study: [2]
| Animal Models | Rat |
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| Dosages | 1-100 μg/kg |
| Administration | i.v. |
| Solubility | Saline, 30 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 236.74 |
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| Formula | C13H16N2.HCl |
| CAS No. | 86347-15-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 12 mg/mL (50 mM) |
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| Water | 47 mg/mL (198 mM) | ||
| Ethanol | 47 mg/mL (198 mM) | ||
| In vivo | Saline, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 1H-Imidazole, 5-[1-(2,3-dimethylphenyl)ethyl]-, hydrochloride (1:1) |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.23674 | 2.3674 | 4.7348 | 7.1022 |
