Dopamine D1/D5 receptor antagonists with improved
Abstract Benzazepines 1 and 2 (SCH 23390 and SCH 39166, respectively) are two classical benzazepine D1/D5 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 Agonists - StatPearls - NCBI Bookshelf
Dopamine agonists, such as ropinirole, are the first-line treatment for restless legs syndrome, while bromocriptine is given for neuroleptic malignant syndrome. Dopamine agonists are also prescribed to counteract dopamine antagonist-induced hyperprolactinemia. Dopamine agonists are used in patients with Parkinson disease.
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...
The Signaling and Pharmacology of the Dopamine D1 Receptor
The dopamine D1 receptor (D1R) is a Gα s/olf -coupled GPCR that is expressed in the midbrain and forebrain, regulating motor behavior, reward, motivational states, and cognitive processes.
Dopamine D1/D5 Receptor Antagonists with Improved
Dopamine D1/D5 Receptor Antagonists with Improved Pharmacokinetics: Design, Synthesis, and Biological Evaluation of Phenol Bioisosteric Analogues of Benzazepine D1/D5 Antagonists Wen-Lian Wu , Duane A. Burnett , Richard Spring , William J. Greenlee , Michelle Smith , Leonard Favreau , Ahmad Fawzi , Hongtao Zhang , and Jean E. Lachowicz
- 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 skf83959 a D1 receptor antagonist?
- Provided by the Springer Nature SharedIt content-sharing initiative SCH23390 is a widely used D1 dopamine receptor (D1R) antagonist that also elicits some D1R-independent effects. We previously found that the benzazepine, SKF83959, an analog of SCH23390, produces positive allosteric modulation of the Sigma-1 receptor (Sig1R).
- Does G(olf)Alpha mediate dopamine D1 receptor signaling?
- G (olf)alpha mediates dopamine D1 receptor signaling. J. Neurosci. 20:Rc91. 10.1523/JNEUROSCI.20-16-j0001.2000 [DOI] [PMC free article] [PubMed] [Google Scholar] Zhuang Y., Xu P., Mao C., Wang L., Krumm B., Zhou X. E., et al. (2021). Structural insights into the human D1 and D2 dopamine receptor signaling complexes.
- 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.
- Can non-catechol D1R agonists be used for neuropsychiatric disorders?
- The emergence of new non-catechol D1R agonists, biased agonists, and allosteric modulators has renewed clinical interest in drugs targeting this receptor, specifically for the treatment of motor impairment in Parkinson's Disease, and cognitive impairment in neuropsychiatric disorders.
- 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]
