Dopamine D1/D5 receptor antagonists with improved
Replacement of the phenol group of 2 with an indole ring generated the first potent D1/D5 antagonist 11b. Further optimization led to the synthesis of very potent benzimidazolones 19, 20 and benzothiazolone analogues 28, 29. These compounds have excellent selectivity over D2-D4 receptors, alpha2a receptor, and the 5-HT transporter.
The Dopamine D5 receptor contributes to activation
The D5 receptor belongs to the D1-type family of dopamine receptors that are coupled via Gα s /Gα olf and initiate cAMP/PKA signaling 10. Compared to the D1 receptor, in most regions...
Mechanisms of D1/D2-like dopaminergic agonist
Rotigotine ([-]2-(N-propyl-N-2-thienylethylamino)-5-hydroxytetraline) is a dopamine agonist with an affinity for all dopamine receptors (D1 to D5), which when delivered daily as a single dose
Dopamine D1/D5 Receptor Antagonists with Improved
Benzazepines 1 and 2 (SCH 23390 and SCH 39166, respectively) are two classical benzazepine D 1 /D 5 antagonists, with Ki values 1.4 and 1.2 nM, respectively. Compound 2 has been in human clinical trials for a variety of diseases, including schizophrenia, cocaine addition, and obesity.
Dopamine Controls Persistence of Long-Term Memory Storage
It has been proposed that VTA/hippocampus connections gate relevant information into LTM through a D1/D5-dependent mechanism . Dopamine modulates late long-term potentiation (LTP) in CA1 , whereas VTA N-methyl-d-aspartate receptors (NMDARs) regulate the development of dopamine-mediated long-term changes in the brain reward circuitry, control
- Does dopamine D5 regulate BDNF and Akt signalling in rodent prefrontal cortex?
- A physiological role for the dopamine D5 receptor as a regulator of BDNF and Akt signalling in rodent prefrontal cortex. Int. J. Neuropsychopharmacol. 16, 477–483. 10.1017/s1461145712000685 [DOI] [PMC free article] [PubMed] [Google Scholar]
- Is SCH 23390 a d1/d5r antagonist?
- However, a limitation of these studies is that they all used intracerebral injection of the D1/D5R antagonist SCH 23390, a drug which also possesses activity at 5-HT2 receptors (Hyttel, 1983; Briggs et al., 1991).
- Does phosphorylation affect D1 dopamine receptor desensitization?
- The role of phosphorylation in D1 dopamine receptor desensitization: evidence for a novel mechanism of arrestin association. J. Biol. Chem. 279, 7999–8010. 10.1074/jbc.M308281200 [DOI] [PMC free article] [PubMed] [Google Scholar] Kimberg D. Y., D'Esposito M. (2003). Cognitive effects of the dopamine receptor agonist pergolide.
- Can drugs directly target the dopamine D1 receptor (D1R)?
- More specifically, drugs that directly target the dopamine D1 receptor (D1R) have been investigated for the treatment of motor impairment in Parkinson's Disease, and cognitive impairment associated with age, neuropsychiatric, and neurodegenerative diseases.
- Is A-77636 a dopamine D1 receptor agonist?
- Kebabian J. W., Britton D. R., DeNinno M. P., Perner R., Smith L., Jenner P., et al. (1992a). A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets.
- Is the dopamine D5 receptor involved in working memory?
- The dopamine D5 receptor is involved in working memory. Front. Pharmacol. 8:666. 10.3389/fphar.2017.00666 [DOI] [PMC free article] [PubMed] [Google Scholar] Carr K. D., Chau L. S., Cabeza de Vaca S., Gustafson K., Stouffer M., Tukey D. S., et al. (2010).
