D₂ Receptor Agonist

MCL-524 is a highly selective full agonist of the dopamine D₂ receptor with a K_d value of 1.34 nM. MCL-524 specifically binds to the high-affinity state of the dopamine D₂ receptor; this binding is abolished by guanylylimidodiphosphate, and it can distinguish between D₂^high and D₂^low sites. MCL-524 is applicable to research related to Parkinson's disease and schizophrenia.

PD 158771 is an antipsychotic agent that functions as a partial agonist for D₂ /D₃ receptors (K_i = 42.0/13.7 nM) and as an agonist for 5-HT_1A receptors (K_i = 2.6 nM). PD 158771 can be utilized in antipsychotic research.

Pramipexole-d₇ dihydrochloride is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with K_is of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).

D-520 is a potent and brain-penetrant dopamine D2/D3 agonist (D2 EC₅₀ = 4.73 nM, K_i = 41.8 nM; D3 EC₅₀ = 2.18 nM, K_i = 0.35 nM). D-520 inhibits the formation of Aβ aggregates in vitro and promotes the disaggregation of both alpha-synuclein (α-syn) and Aβ aggregates. D-520 exhibits efficacious activity in animal models of Parkinson’s disease (PD). D-520 can be used for PD and PD with dementia (PDD) research^[1][2].

Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.

BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (K_i=0.92 nM) and a 70 times lower affinity at the D2 receptor (K_i=61 nM).

Tau-aggregation-IN-1 (Compound D-519) is a tau441 protein aggregation inhibitor with an IC₅₀ of 21 µM. Tau-aggregation-IN-1 is also a dopamine D₂ and D₃ receptor agonist.

Dopamine D2 receptor agonist-4 is a blood-brain barrier permeable Dopamine D2 receptor agonist with an EC₅₀ value of 0.03 nM. Dopamine D2 receptor agonist-4 reduces intracellular cAMP levels. Dopamine D2 receptor agonist-4 acts as a Ferroptosis inhibitor and iron chelator, selectively chelating iron ions, reducing intracellular ferrous ion levels, and exerting cytoprotective effects against iron-dependent ferroptosis in vitro. Dopamine D2 receptor agonist-4 improves motor dysfunction and exerts neuroprotective effects in mouse models of Parkinson's disease. Dopamine D2 receptor agonist-4 can be used in studies related to Parkinson's disease.

5-OH-DPAT (5-Hydroxy-DPAT) is a potent and selective dopamine D2-receptor agonist lacking effects at 5-HT receptors. 5-OH-DPAT produces a moderate facilitation of the male rat sexual behavior.

Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM).

CNV-dopamine is a photoreleasable D2 receptor-selective agonist. CNV-dopamine activates D2 receptors and induces G protein-coupled inwardly rectifying potassium (GIRK) currents. CNV-dopamine is promising for research of disorders like Parkinson’s disease and addiction.

Lirexapride is a 5-HT4/Dopamine D2 receptor agonist. Lirexapride stimulants gastrointestinal motor. Lirexapride can be used for research on digestive system disorders.

Carmoxirole (EMD 45609) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo.

5-HT2A receptor agonist-13 (Compound 28c) is a partial agonist of the 5-HT_2A receptor, with an EC₅₀ value of 416.9 nM and a K_i value of 113.9 nM. 5-HT2A receptor agonist-13 exhibits very weak agonistic activity towards the 5-HT_2B receptor (EC₅₀ = 120.2 nM), D2 receptor (K_i = 1298 nM), and has no activity towards the 5-HT_2C receptor. 5-HT2A receptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC₅₀ = 977.2 nM). 5-HT2A receptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2A receptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD).

Bromocriptine-¹³C,d₃ is the ¹³C- and deuterium labeled Bromocriptine. Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.

Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pK_is of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC₅₀ of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia.

Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.

PD 118717 is a selective dopamine (DA) D-2 autoreceptor agonist. PD 118717 has significant affinity for 5-HT1A but not 5-HT1B and 5-HT2 receptors. PD 118717 is active in antagonizing the tau-Butyrolactone-induced accumulation of dopa in rat striatum and mesolimbic regions. PD 118717 exhibits an antipsychotic-like profile.

AB13-46A is a selective dopamine receptor agonist, with a K_i value of 0.505 nM against human D₃R. AB13-46A can be used for research on nervous system-related diseases.

PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with K_i values of 25.5 nM and 16.6 nM for human D2 and D3 receptors, respectively and lower affinity for D4.2 receptors (K_i=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology.