D₂ Receptor Agonist

Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pK_i of 8.05. Bromocriptine mesylate is permeable to the blood-brain barrier.

Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

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.

Brexpiprazole (OPC-34712), 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 is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM).

Cabergoline is an ergot derived-dopamine D₂-like receptor agonist that has high affinity for D₂, D₃, and 5-HT_2B receptors (K_i=0.7, 1.5, and 1.2, respectively).

Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.

Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED₅₀ of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome.

Ropinirole (SKF 101468) hydrochloride is an orally active, potent D₃/D₂ receptor agonist with a K_i of 29 nM for D₂ receptor. Ropinirole hydrochloride has pEC₅₀s of 7.4, 8.4 and 6.8 for hD₂, hD₃ and hD₄ receptors, respectively. Ropinirole hydrochloride has no affinity for the D₁ receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.

Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_i of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

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).

Pramipexole 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 can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).

Lisuride is an orally active dopamine D2 receptors agonist. Lisuride, as an ergot derivative, can be used for the research of Parkinson's disease, migraine, and high prolactin levels.

UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D₂ receptor (D₂R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a K_i of 79 nM for D₂R. UNC9994 hydrochloride is also an antagonist of G_i-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.

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

Pramipexole dihydrochloride hydrate 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 hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).

Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D₂/D₃ receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin 5-HT₁A, 5-HT₂A and 5-HT₂B receptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole.

Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.

MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (K_i=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC₅₀=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC₅₀=9.9 μM).

UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions.