d1 receptor

D1/D5 Receptor agonist-1 is an orally active D1/D5 receptor agonist with the ability to cross the blood-brain barrier. It demonstrates significant efficacy in the cAMP pathway and β-arrestin recruitment, with EC50 values of 3.7 nM for D1R cAMP, 91 nM for D1R β-arrestin, and 129 nM for D1R internalization, and a Ki value of 111 nM for D1R binding affinity. In rats, D1/D5 Receptor agonist-1 inhibits β-arrestin signaling involved in L-DOPA-induced dyskinesia. This compound is applicable in Parkinson's disease research.

dopamine D1 receptor antagonist

NGD 94-1 is a selective D4 receptor antagonist with an affinity of 3 nM for the D4 receptor and greater than 2 pM for the D1, D2, D3, and D5 receptors.NGD 94-1 can be used in the study of cognitive disorders and other psychiatric disorders.

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease.

Romergoline 2HCl is a D1 agonist and D2 antagonist used in the study of Parkinson's disease.

BP 897 is a potent and selective agonist of dopamine D3 receptor and it is a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors. Which shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 μM, respectively).

UCM-1306 is a potent and orally active allosteric modulator (PAM) of the human dopamine D1 receptor. It increases the maximal effect of endogenous dopamine (DA) in both human and mouse D1 receptors. UCM-1306 could improve motor symptoms and address key comorbid cognitive impairment associated with long-term Parkinson's disease (PD).

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist, specifically targeting D1 and D5 receptors with Ki values of 0.2 nM and 0.3 nM, respectively.

Chlorprothixene (Truxal) is a typical antipsychotic drug of the thioxanthene class, which was the first of the series to be synthesized.

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

Dopamine hydrochloride (ASL279) is a natural catecholamine neurotransmitter that mainly acts on dopamine receptors (D1-5 receptors) (EC50=2.7 nM). Dopamine hydrochloride induces VEGFR2 endocytosis through D2 dopamine receptor and has pro-angiogenic activity.

Rotundine (Gindarine) (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.

Perospirone (Lullan) is an antagonist of serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

Perospirone hydrochloride (Perospirone HCl) is an atypical antipsychotic agent for the treatment of schizophrenia. It also displays affinity towards 5HT1A receptors as a partial agonist.

Chlorprothixene hydrochloride (Truxal hydrochloride) brings strong blocking effects by blocking the 5-HT2 D1, D2, D3, histamine H1, muscarinic and alpha1 adrenergic receptors. Chlorprothixene hydrochloride s a typical antipsychotic drug of the thioxanthene (tricyclic) class.

Blonanserin (AD-5423) is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension.

Blonanserin is an antagonist of dopamine-D2 and serotonin-S2.

LY3154207 is a subtype selective, potent, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).

PF-06256142 is a potent and selective orthosteric D1 receptor agonist(D1 EC50=30 nM ).

Pimozide D4 is a deuterium labeled Pimozide.

(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine, a full agonist of the dopamine receptor and a partial agonist of the 5-HT1A receptor.

(+)-Dihydrexidine hydrochloride is an agonist of dopamine D1 receptor(EC50 of 72± 21 nM).

Dihydrexidine is a full efficacy D1-like dopamine receptor (D1/D5) agonist (IC50: 10 nM for D1 receptor). It also shows potent antiparkinsonian activity.

PF2562 is a dopamine D1 ligand. It is used as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor (Ki: 113 nM). PF2562 shows activity against human D1 cAMP (EC50: 568 nM in HTRF assay).