D₁ Receptor Agonist

SKF 38393 hydrochloride is a selective agonist of the dopamine D1 receptor (D1DR) with an IC₅₀ of 110 nM.

SKF 81297 is a potent and selective dopamine D1 receptor agonist.

SKF 81297 hydrobromide is a potent and selective dopamine D1 receptor agonist.

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.

Fenoldopam (SKF-82526) mesylate is a selective dopamine D₁ receptor agonist. Fenoldopam mesylate binds to rat D₁B dopamine receptors (K_d = 11 nM) and human D₁A receptors (K_d = 17 nM) in COS-7 cell membranes expressing the cloned receptors. Fenoldopam mesylate modulates dopamine receptor expression, induces vasorelaxation in vascular tissues, reverses glomerular hyperfiltration in rat models, increases intracellular cAMP levels, promotes DARPP-32 phosphorylation in small cell lung cancer (SCLC) cells, inhibits cytokine secretion, and downregulates T cell activation markers in activated human T cells. Fenoldopam mesylate can be used for research on hypertension, acute kidney injury, psoriasis, and small cell lung cancer.

N-Methyldopamine hydrochloride is a precursor of adrenaline in the adrenal medulla. N-Methyldopamine hydrochloride is a modification of the dopamine (DA), and retains agonist activity at the DA1 receptor. N-Methyldopamine hydrochloride remains capable of universal surface coating and secondary reactions using the surface catechols. N-Methyldopamine hydrochloride can be used for heart failure research.

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.

SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K_0.5=4 nM), displays selective for D1 over D2 receptors (K_0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC₅₀=491 nM).

Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC₅₀ of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity. Dihydrexidine hydrochloride can stimulate YAP phosphorylation.

A68930 hydrochloride, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis.

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.

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.

SKF 83822 is an atypical agonist of dopamine D1 receptor. SKF 83822 activates adenylyl cyclase (AC), but not phospholipase C (PLC). SKF 83822 is also proved to stimulate AC via cAMP production. SKF 83822 can be used for research of schizophrenia.

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.

CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity.

(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC₅₀=0.8 nM; β-arrestin2, EC₅₀=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.

PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC₅₀ and K_i of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.

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.

DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC₅₀ of 5.8 nM and a K_b of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor.

MLS1082 is a pyrimidone-based D1-like dopamine receptor positive allosteric modulator, with an EC₅₀ of 123 nM for DA-stimulated G protein signaling.