D₂ Receptor Agonist

Sibenadet (AR-C68397AA free base) is a dual dopamine D₂/β₂-adrenoceptor agonist with selective β₂-adrenoceptor agonism. Sibenadet inhibits capsaicin-induced plasma protein extravasation in rat trachea. Sibenadet suppresses edema from sensory nerve fiber activation by activating β₂-adrenoceptor. Sibenadet is promising for research of chronic obstructive pulmonary disease (COPD).

Roxindole (EMD 49980), 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. Antipsychotic and antidepressant activities.

Dopamine D3 receptor agonist-2 is a selective dopamine D3 receptor partial agonist with a K_i of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamine D2 receptor (K_i= 7.67nM).

(-)-IHCH7041 (Compound (-)-(S)-I-10) is a selective and orally active dopamine D2 receptor agonist with a K_i of 22.44 nM. (-)-IHCH7041 can activate Gαi1 protein and β-arrestin2 signaling pathway with EC₅₀ values of 1.38 and 2.75 nM. (-)-IHCH7041 can improve cognitive impairment and memory capacity. (-)-IHCH7041 can be used for the research of neurological disease, such as Alzheimer's disease.

RU-24213 hydrochloride is a selective D-2 dopamine receptor agonist. RU-24213 hydrochloride is also a KAPPA-opioid receptor antagonist. RU-24213 hydrochloride induces stereotyped behaviors.

AB12-82 is a selective dopamine receptor agonist with a K_i value of 1.88 nM for human D₃R. AB12-82 achieves subtype-selective D₃R activation by enhancing interactions with the D₃R H291·32 residue. AB12-82 can be used in the research of nervous system-related diseases.

Cabergoline-d₆ is 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).

D2R/D3R/5-HT1AR agonist 1 (compound 22b) is an orally active triple-target D2R/D3R/5-HT1AR agonist with EC₅₀ values of 1.29, 1.05 and 153.5 nM. D2R/D3R/5-HT1AR agonist 1 can improve the behavioral disorders induced by MPTP (HY-W114750) and exerts anti-depression effect. D2R/D3R/5-HT1AR agonist 1 can be used for the research of Parkinson's disease and depression.

OS-3-106 is a potent, and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (K_i = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research.

AB13-08 is a selective dopamine receptor agonist with a K_i value of 53.9 nM for human D₃R. AB13-08 is applicable to the research of neurological disorders such as Parkinson's disease and schizophrenia.

Alentemol (U-66444B (free base)) is a blood-brain barrier-permeable dopamine receptor D₁, D₂, D₃, and D₄ agonist. Alentemol inhibits dopamine release, reduces dopamine synthesis, regulates dopamine metabolism, suppresses the impulse activity of dopaminergic neurons, and decreases the impulse frequency of dopaminergic neurons in the substantia nigra pars compacta and ventral tegmental area. Alentemol is applicable to research related to schizophrenia.

Sumanirole (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.

FAUC-312, a tetrahydropyrimidine, is a strong and highly selective dopamine D4 receptor partial agonist (K_i=1.5 nM).

Pardoprunox (SLV-308) 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.

MS1768 is a G protein-biased, partial, and selective D2R agonist. MS1768 selectively activates the Gi/o signaling pathway rather than recruiting β-arrestin2. MS1768 inhibits hyperkinesia. MS1768 can be used in studies of hyperkinesia.

Dopamine D3 receptor ligand-5 (13a), a Cariprazine (HY-14763) analogue, is a dopamine D3 receptor ligand, with K_i values of 2.85 nM and 0.14 nM for D₂R and D₃R, respectively.

Alentemol hydrobromide (U-66444B) is a blood-brain barrier-permeable dopamine receptor D₁, D₂, D₃, and D₄ agonist. Alentemol hydrobromide inhibits dopamine release, reduces dopamine synthesis, regulates dopamine metabolism, suppresses the impulse activity of dopaminergic neurons, and decreases the impulse frequency of dopaminergic neurons in the substantia nigra pars compacta and ventral tegmental area. Alentemol hydrobromide is applicable to research related to schizophrenia.

Cariprazine impurity 1 is a dopamine D2 receptor (D2R) agonist. Cariprazine impurity 1 modulates D2R-mediated G_i/o signaling pathway to inhibit cAMP production, and regulates D2R-mediated β-arrestin2 recruitment pathway.

FR 64822 is a dopamine D2 receptor agonist that can induce antinociceptive activity in rats and mice by indirectly stimulating dopamine D2 receptors. FR 64822 can promote penile erection in juvenile rats and improve amnesia in rats induced by scopolamine during passive avoidance tasks.