D₂ Receptor Modulator

Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D₃ (K_i=0.085 nM) and D₂ (K_i=0.49 nM) receptors, and moderate affinity for the 5-HT_1A receptor (K_i=2.6 nM).

Cariprazine hydrochloride is a novel antipsychotic agent candidate that exhibits high affinity for the D₃ (K_i=0.085 nM) and D₂ (K_i=0.49 nM) receptors, and moderate affinity for the 5-HT_1A receptor (K_i=2.6 nM).

Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

Neuromedin N is a potent modulator of dopamine D2 receptor agonist binding in rat neostriatal membranes.

L-Stepholidine (Stepholidine) is an alkaloid. L-Stepholidine exhibits mixed dopamine D1 receptor agonist and D2 antagonist properties. L-Stepholidine has neuroprotective effect. L-Stepholidine can be used for the researches of neurological disease, such as Parkinson disease, Alzheimer's disease and opiate addiction.

PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists.

AL-LAD (6-Allyl-6-nor-LSD) is an activator for 5-HT2A receptor with K_i of 3.4-8.1 nM. AL-LAD exhibits affinity for dopamine receptor D1 and dopamine receptor D2 with absolute affinitiesK_0.5 of 189 nM and 12.3 nM. AL-LAD acts as psychoactive substance in mouse model.

5-HT_1AR agonist 2 (Compound 4f) is a 5-HT_1A receptor agonist (K_i: 10.0 nM). 5-HT_1AR agonist 2 also binds to the SERT, D₂ receptor and 5-HT₆ receptor (K_i: SERT, 2.8 nM; D₂, 23 nM; 5-HT₆, 192 nM). 5-HT_1AR agonist 2 is stabilized in microsomes and induces hypothermia in mice.

Nooglutil (Nooglutyl; ONK-10) is a positive modulator of AMPA-type glutamate receptors (AMPARs). Nooglutil also regulates dopamine D2 receptor function to exert anxiolytic effects. Nooglutil is promising for research of neurodegenerative disorders (e.g., Alzheimer’s disease).

BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride 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).

Dopamine D2 receptor agonist-3 (compound 3) is a selective D2 receptor partial agonist and Dopamine D3 receptor antagonist (with pEC₅₀ of 8.3 and <5.5 respectively).

Dopamine D2 receptor modulator-1 is a positive allosteric modulator of hD2R. Dopamine D2 receptor modulator-1 enhances the potency of Dopamine (HY-B0451) on hD2R without intrinsic agonist activity. Dopamine D2 receptor modulator-1 protects dopaminergic differentiated cells from neurotoxic damage. Dopamine D2 receptor modulator-1 exhibits neuroprotective activity. Dopamine D2 receptor modulator-1 can be used in the research of Parkinson's disease.

5-HT₇R antagonist 3 (Compound 6.4) is a selective 5-HT₇R antagonist (K_i: 8 nM), with K_i of 511 nM (D₂), 8930 nM (5-HT_1A) and 5786 nM (5-HT_2A), respectively. 5-HT₇R antagonist 3 possesses antidepressant and anxiolytic effects in mice.