Uses
SKF-83959 was used in dopamine signaling studies on eye blinking in monkeys and on phosphorylation of CaMKIIα in mice.
Definition
ChEBI: A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine bearing a 3-methylphenyl substituent at position 1, a methyl substituent at position 3, a chloro substituent at position 6 and two hydroxy substituents at positions 7 and 8. Dopamine D1-like receptor p
rtial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). May act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonising the behavioral effects of cocaine.
Biological Activity
Dopamine D 1 -like receptor partial agonist (K i values are 1.18, 7.56, 920 and 399 nM for rat D 1 , D 5 , D 2 and D 3 receptors respectively). May act as an antagonist in vivo , producing antiparkinsonian effects and antagonizing the behavioral effects of cocaine.
in vivo
SKF83959 (0.5 and 1 mg/kg; i.p.; 1 hour) reverses the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test[1].
SKF83959 (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade[1].
SKF83959 has anti-amnesic activities and restores the scopolamine-decreased BDNF signaling pathway in the hippocampus in mice[1].
| Animal Model: | Male ICR male mice (8 weeks)[1] |
| Dosage: | 0.5 and 1 mg/kg |
| Administration: | I.p.; 1 hour |
| Result: | Reversed the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test.
|
| Animal Model: | Male ICR male mice (8 weeks)[1] |
| Dosage: | 1 mg/kg |
| Administration: | I.p.; 30 minutes |
| Result: | The memory enhancing effects were prevented by BDNF system blockade.
|
IC 50
D
1 Receptor: 1.18 nM (Ki); Sigma 1 Receptor; D
5 Receptor: 7.56 nM (Ki); D
2 Receptor: 920 nM (Ki); D
3 Receptor: 399 nM (Ki)
