D₄ 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).

ABT-724 trihydrochloride is a potent and highly selective dopamine D₄ receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D₄ receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D₄ (EC₅₀ of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM), and has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.

(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.

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).

Ro 10-5824 is a potent and selective D4R partial agonist with a K_i of 5.2 nM. Ro 10-5824 increases novel object exploration in C57 mice.

PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with K_i values of 25.5 nM and 16.6 nM for human D2 and D3 receptors, respectively and lower affinity for D4.2 receptors (K_i=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology.

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).

U-99363E is a selective dopamine D4 receptor antagonist with a K_i value of 2.2 nM. U-99363E exhibits at least 100-fold lower affinity for other dopaminergic, serotonergic and adrenergic receptors. U-99363E can be used in studies related to selective dopamine D4 site labeling or blockade.

(Rac)-Rotigotine-d₇ (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (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 Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the K_i of 1.6 nM. FGH31 partial activates β- arrestin.

ABT-724, a chemical probe, is a potent and highly selective dopamine D₄ receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D₄ receptor. ABT-724 is a potent partial agonist at the rat D₄ (EC₅₀ of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM). ABT-724 has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.

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.

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

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.

ABT-670 is a selective, oral bioavailable agonist of dopamine D₄ receptor, with EC₅₀ of 89 nM, 160 nM, and 93 nM for human D₄, ferret D₄, and rat D₄, respectively.