SKF 81297 hydrobromide
SKF 81297 hydrobromide is a selective agonist of the dopamine D1-like receptor, with a Ki value 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.
| 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 |
| SDF | Download SDF |
| Canonical SMILES | ClC1=C2C([C@@H](C3=CC=CC=C3)CNCC2)=CC(O)=C1O.Br |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Animal experiment:[3] | |
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Animal models |
1-Methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP)-lesioned parkinsonian rhesus monkeys |
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Dosage form |
0.3 mg/kg Injected intramuscularly |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
