D₂ Receptor Agonist

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

Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT_1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT_1A (IC₅₀=0.9 nM). Antipsychotic and antidepressant activities.

Sarizotan (EMD 128130) is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively.

UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC₅₀ <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of G_i-regulated cAMP production. Antipsychotic Activity.

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

Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.

Pergolide (LY127809 free base), an Ergoline derivative, is a potent and orally active dopamine D₁ and D₂ receptor agonist. Pergolide can be used for Parkinson's disease and hyperprolactinaemia research.

Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD).

Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D₂ and D₃ receptors, full agonist at the 5-HT_1A receptor, and antagonist at the human 5-HT_2B receptor (K_i: 1.41 nM (human D_2L), 0.056 nM (human D₃), 1.7 nM (human 5-HT_1A), 0.52 nM (human 5-HT_2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.

Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate 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 monohydrate can be used for the research of schizophrenia and COVID19.

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).

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

A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pK_i=7.40; K_i=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor.

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.

Aplindore (DAB-452) is a potent agonist of the dopamine D2 receptor, with the pK_i of 9.1. Aplindore plays an important role in Parkinson's disease research.

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).