D₃ Receptor Agonist

Pramipexole-d₅ dihydrochloride is 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).

SKF83959 hydrobromide is a potent and selective dopamine D₁-like receptor partial agonist. SKF83959 hydrobromide K_i values for rat D₁, D₅, D₂ and D₃ receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression.

Pardoprunox (SLV-308) hydrochloride is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC₅₀s of 8, 9.2, and 6.3, respectively.

Quinelorane dihydrochloride (LY163502) is a potent dopamine D3/D2 receptor agonist. Quinelorane has the potential for neurological and psychiatric disorders research.

ST-836 hydrochloride (compound 34) is a potent dopamine receptor ligand with K_i values of 4.5 nM, 132 nM for D3 and D2, respectively. ST-836 hydrochloride has the potential for Parkinson’s disease.

(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine 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_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

Cabergoline-d₅ is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).

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).

SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC₅₀ of 1109 nM. SK609 hydrochloride has the potential for parkinson research.

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].

ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC₅₀ = 15.2 nM, K_i =1.5 nM) and potent GSK-3β inhibitor activity (IC₅₀ = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.

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.

AB13-73A is a highly selective partial agonist of dopamine D₃R, with a K_i of 0.803 nM and a pEC₅₀ of 11.88 (1.32 pM). AB13-73A serves as a pharmacological tool to dissect the (patho) physiological mechanisms of D₃R and support the development of improved neurotherapeutic agents.

FAUC 346, a highly selective D₃ partial agonist (EC₅₀ = 1.5 nM).

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.

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.

Obuprazine is an orally active dopamine D3 receptor agonist and 5-HT2A receptor antagonist with IC₅₀ values of 0.37 and 4.19 nM, respectively. Obuprazine acts as a G protein-coupled receptor modulater. Obuprazine can be used for the research of schizophrenia.