| CAS NO: | 104054-27-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 212.29 |
|---|---|
| Formula | C14H16N2 |
| CAS No. | 104054-27-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 42 mg/mL (197.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: 42 mg/mL (197.8 mM) | |
| Other info | Chemical Name: 1H-Imidazole, 4-(2-ethyl-2,3-dihydro-1H-inden-2-yl)- InChi Key: HSWPZIDYAHLZDD-UHFFFAOYSA-N InChi Code: InChI=1S/C14H16N2/c1-2-14(13-9-15-10-16-13)7-11-5-3-4-6-12(11)8-14/h3-6,9-10H,2,7-8H2,1H3,(H,15,16) SMILES Code: CCC1(C2=CNC=N2)CC3=C(C=CC=C3)C1 |
| Synonyms | Antisedan, MPV-1248, MPV1248, MPV 1248 |
| In Vitro | In vitro activity: The alpha2-adrenoceptor antagonist atipamezole was a potent inhibitor of aldosterone release (range 10-1000 nM). In receptor binding studies [( 3H]-clonidine and [3H]-prazosin displacement) an alpha 2/alpha 1 selectivity ratio of 8526 was obtained for atipamezole, while idazoxan and yohimbine showed ratios of 27 and 40, respectively. Atipamezole had also about a 100 times higher affinity on alpha 2-adrenoceptors than the reference compounds. Kinase Assay: Atipamezole Hcl(MPV1248 Hcl) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor. |
|---|---|
| In Vivo | In vivo studies of [3H]atipamezole demonstrated good penetration into the brain (0.3-1.8% injected dose/g at 5 min, depending upon brain region). In addition, [3H]atipamezole displayed rapid in vivo clearance of nonspecific binding such that at 1 h following an i.v. injection of the drug (100 microCi/animal, rat tail vein administration) the pattern of radioactivity in the brain correlated very well with the receptor distribution as seen by in vitro autoradiography. In mice, medetomidine-induced sedation was effectively antagonized by atipamezole. |
| Animal model | Rats |
| Formulation & Dosage | i.v. injection of the drug (100 microCi/animal, rat tail vein administration) |
| References | J Neural Transm Park Dis Dement Sect. 1992;4(2):99-106; Eur J Pharmacol. 1998 Apr 3;346(1):71-6; Eur J Pharmacol. 1992 Nov 24;224(1):27-38. |
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