CAS NO: | 67287-39-2 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 370.67 |
Cas No. | 67287-39-2 |
Formula | C16H16ClNO2·HBr |
Solubility | Soluble in DMSO |
Chemical Name | (R)-6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrobromide |
Canonical SMILES | ClC1=C2C([C@@H](C3=CC=CC=C3)CNCC2)=CC(O)=C1O.Br |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
SKF 81297 hydrobromide is a selective agonist of the dopamine D1-like receptor, with aKivalue of 1.9 nM. The dopamine D1-like receptors, consisting of D1 and D5 subtypes, are a subfamily of dopamine receptors that mediate excitatory neurotransmission after binding the endogenous neurotransmitter dopamine. The dopamine D1-like receptors have been implicated in dopaminergic regulation of a variety of fundamental neurophysiologic processes including mood, motivation, cognitive function, as well as motor activity.
References:
1. Neumeyer JL, Kula NS, Bergman J, Baldessarini RJ. Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. European Journal of Pharmacology, 2003, 474(2-3): 137-140.
2. Undieh AS. Pharmacology of signaling induced by dopamine D(1)-like receptor activation. Pharmacology & Therapeutics, 2010, 128(1): 37-60.
3. Vermeulen RJ, Drukarch B, Sahadat MC, et al. The dopamine D1 agonist SKF 81297 and the dopamine D2 agonist LY 171555 act synergistically to stimulate motor behavior of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned parkinsonian rhesus monkeys. Movement Disorders, 1994, 9(6): 664-672.
Animal experiment:[3] | |
Animal models | 1-Methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP)-lesioned parkinsonian rhesus monkeys |
Dosage form | 0.3 mg/kg Injected intramuscularly |
Applications | Coadministration of behaviorally active doses of the dopamine D1 agonist SKF 81297 (0.3 mg/kg) and the dopamine D2 agonist LY 171555 (0.01 mg/kg) resulted in a prolongation of the motor stimulation induced by either of the drugs alone. Neither administration of SKF 81297, in a dose of 0.03 mg/kg, nor of LY 171555, in a dose of 0.003 mg/kg, were behaviorally active, whereas the combined administration of these compounds induced a significant stimulation of motor behavior. |
Note | The technical data provided above is for reference only. |
References: 1. Mancini JA, Prasit P, Coppolino MG, et al. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Molecular Pharmacology, 1992, 41(2): 267-272. 2.Dixon RA, Diehl RE, Opas E, et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature, 1990, 343(6255): 282-284. 3. Kehrer JP, Biswal SS, La E, et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochemical Journal, 2001, 356(Pt 3): 899-906. 4. Imbesi M, Zavoreo I, Uz T, et al. 5-Lipoxygenase inhibitor MK-886 increases GluR1 phosphorylation in neuronal cultures in vitro and in the mouse cortex in vivo. Brain Research, 2007, 1147: 148-153. |