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Merck

S179

Sigma-Aldrich

R(+)-SKF-81297 hydrobromide

≥98% (HPLC), solid

别名:

R-(+)-6-Chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide

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About This Item

经验公式(希尔记法):
C16H16ClNO2 · HBr
分子量:
370.67
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

solid

光學活性

[α]22/D +15.14°, c = 0.52 in DMF(lit.)

儲存條件

desiccated
protect from light

顏色

white to off-white

溶解度

H2O: 6 mg/mL
DMSO: soluble

SMILES 字串

Br[H].Oc1cc2[C@H](CNCCc2c(Cl)c1O)c3ccccc3

InChI

1S/C16H16ClNO2.BrH/c17-15-11-6-7-18-9-13(10-4-2-1-3-5-10)12(11)8-14(19)16(15)20;/h1-5,8,13,18-20H,6-7,9H2;1H/t13-;/m1./s1

InChI 密鑰

RMIJGBMRNYUZRG-BTQNPOSSSA-N

應用

R(+)-SKF-81297 hydrobromide has used as D1-type dopamine receptor agonist:
  • to test it effect on the spike firing in rat retinal ganglion cells
  • in human embryonic kidney (HEK) 293T cells
  • to test its inhibitory effect in microglial cells

生化/生理作用

SKF-81297 administration in spontaneously hypertensive rats (SHR) induces an increase in expression of proto-oncogene c-fos mRNA leading to biphasic effect on locomotion. It favors the turnover of phosphoinositide and adenylyl cyclase. SKF-81297 is involved in the stimulation of neurons, in particular the postsynaptic striatal neurons.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


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R J Vermeulen et al.
European journal of pharmacology, 235(1), 143-147 (1993-04-22)
The alleged selective, high efficacy dopamine D1 receptor agonist, SKF 81297 (0.05-0.3 mg/kg i.m.), induced rotational behaviour away from the lesion and stimulated use of the dominant right hand in unilaterally (left side) 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned rhesus monkeys (Macaca mulatta). The
C. Reavill et al.
Behavioural pharmacology, 4(2), 135-146 (1993-04-01)
A range of selective dopamine D1 and D2 receptor agonists and antagonists was used to characterize to the discriminative stimuli produced by d-amphetamine (0.5mg/kg) and the D1 agonists SKF 81297 (0.1mg/kg). In rats trained to discriminate d-amphetamine (0.5mg/kg) from saline
Asim J Rashid et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(2), 654-659 (2006-12-30)
We demonstrate a heteromeric D1-D2 dopamine receptor signaling complex in brain that is coupled to Gq/11 and requires agonist binding to both receptors for G protein activation and intracellular calcium release. The D1 agonist SKF83959 was identified as a specific
J Bergman et al.
The Journal of pharmacology and experimental therapeutics, 273(1), 40-48 (1995-04-01)
The effects of dopamine agonists differing in affinity and selectivity at D1 and D2 types of dopamine receptors were compared in squirrel monkeys responding under two different schedules of reinforcement: a fixed-interval (FI) schedule of stimulus-shock termination and a fixed-ratio
Mauricio Dos-Santos-Pereira et al.
Glia, 66(11), 2353-2365 (2018-11-06)
When activated, microglial cells have the potential not only to secrete typical proinflammatory mediators but also to release the neurotransmitter glutamate in amounts that may promote excitotoxicity. Here, we wished to determine the potential of the Parkinson's disease (PD) protein

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