1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE3-Methoxytyramine hydrochlorideCat. No.: HY-103638CAS No.: 1477-68-5Synonyms: 3-O-methyl Dopamine hydrochloride分式: CHClNO分量: 203.67作靶點: Drug Metabolite作通路: Metabolic Enzyme/Protease儲存式: -20C, protect from light* In solvent : -80

2、C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (490.99 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.9099 mL 24.5495 mL 49.0990 mL5 mM 0.9820 mL 4.9099 mL 9.8198 mL10 mM 0.4910 mL 2.4550 mL 4.9099 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液

3、的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (12.27 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility:

4、 2.5 mg/mL (12.27 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (12.27 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 3-Methoxytyramine hydrochloride多巴胺的活性代謝物，可以活化痕量胺相關受體1 (TAAR1)。IC50 & Target TAAR1 1體外研究 The intensity of the

5、 fluorescence developed is in a linear relation to the amount of 3-Methoxytyraminehydrochloride presented in the sample up to at least 1 g. When a high concentration of dopamine is presentin the reaction mixture, there is some reduction in the fluorescence derived from 3-Methoxytyraminehydrochloride

6、 1.體內(nèi)研究 The extracellular DA metabolite 3-Methoxytyramine hydrochloride (3-MT) induces significant behavioralactivation in DDD mice. This activity however, is mostly presented as a set of disorganized abnormalmovements that includes tremor, head bobbing, straub tail, grooming and abnormal orofacial

7、movementsrather than normal forward activity. No effect is observed when 3-Methoxytyramine hydrochloride is infusedat doses below 9 g, at 9 g and higher doses 3-Methoxytyramine hydrochloride dose-dependently causestransient behavioral activation with a complex set of behaviors. In particular, transi

8、ent hyperactivity andstereotypy, sniffing, grooming, rearing and mild abnormal involuntary movements (AIMs) at the level of limbsis observed after infusion of 9 g of 3-Methoxytyramine hydrochloride. Similar behaviors are also observedafter 18 g of 3-Methoxytyramine hydrochloride with the additional

9、appearance of tremor as well as oral andwhole body AIMs 1.PROTOCOLCell Assay 1 The rats are killed by cervical dislocation and the brains are removed and placed on an ice-cooled glassplate. The corpora striata are dissected out and homogenized immediately or stored at -17C until analyzed.For the est

10、imation of 3-Methoxytyramine hydrochloride 1 mL of the neutralized perchloric acid solution isplaced in a glass test tube. One millilitre of a solution of potassium ferricyanide (20 g/mL) in concentratedammonium hydroxide is added. After 2 min 0 to 1 mL of a solution of cysteine (1 mg/mL) is added a

11、nd mixed.The fluorescence of the resulting solution is measured in a spectrophotofluorometer fitted with aninterference filter in the fluorescence light path. A blank determination is made by reversing the order of theaddition of the ferricyanide-ammonia solution and the solution of cysteine. Authen

12、tic 3-Methoxytyraminehydrochloride is also added to a portion of the neutralized eluate and the fluorescence developed to check forquenching 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal To assess effects of 3-Methoxytyramine hydrochloride (3

13、-MT) in normal and TAAR1-KO mice, the animalsAdministration 1 are placed in the locomotor activity chamber and 30 min later various doses of 3-Methoxytyraminehydrochloride are administered i.c.v. To perform i.c.v. administration in this paradigm, habituated mice areremoved from the experimental cham

14、ber, briefly restrained, i.c.v. injection cannula is placed into thepreviously implanted (one week before) guide cannula and infusion of 3-Methoxytyramine hydrochloride orvehicle is performed for 4 minutes when animal is freely moving in a home cage. After infusion, animals are2/3 Master of Small Mo

15、lecules 您邊的抑制劑師www.MedChemEput back into experimental chamber and behavior is monitored for 90 min after administration 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Sotnikova TD, et al. The dopamine metabolite 3-methoxytyramine is a neuromodulator. PLoS One. 2010 Oct 18;5(10):e13452.2. Guldberg HC, et al. Some observations on the estimation of 3-methoxytyramine in brain tissue. Br J P