GSK598809 hydrochloride is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

(–)-IHCH7041 is a potent, selective partial agonist at DRD2/3 and 5-HT1AR, EC50 of 1.38 nM in Gαi1–γ9 dissociation and 2.75 nM in β-arrestin2 recruitment assays, with negligible 5-HT2AR binding (>100-fold selectivity).(–)-IHCH7041 exhibits negligible affinities for a large number of tested GPCRs, ion channels and transporters (Ki>500 nM), good affinities for DRD2 and DRD3 (Ki=14.42 nM), and moderate binding to 5-HT1A (Ki=60.62 nM).(–)-IHCH7041 behaves as a partial agonist in both G-protein signaling and β-arrestin recruitment activities at DRD2, DRD3 and 5-HT1AR.(–)-IHCH7041 displayed potent antipsychotic activity and has antidepressant properties and reverses cognitive impairmentin mice.

CJ-1639 (CJ1639) is a potent, highly selective dopamine D3 receptor (D3R) full agonist with Ki of 0.5 nM, >5,000-fold selectivity over D1 and D2 receptors in binding assays.CJ-1639 binds to human D3 receptor with a K(i) value of 3.61 nM and displays over >1000-fold selectivity over human D1 and D2 receptors.CJ-1639 is an excellent pharmacological tool to elucidate the role of the D3 receptor in different neurological conditions in animal models.

PF-06669571 (PF 6669571) is a novel dopamine D1 receptor (D1R) partial agonist with Ki of 10 nM, demonstrates efficacy in pre-clinical models of Parkinson’s disease symptoms.

WW-III-55 is a high-affinity, selective dopamine D3 receptor (D3R) partial agonist with Ki value of 20 nM, exhibits >800-fold binding selectivity for D3R compared with the D2R.WW-III-55 (0-5.6 mg/kg) reduced cocaine self-administration, also reduced responding for sucrose and locomotor activity.WW-III-55 attenuated yawning induced by low doses of 7-OH-DPAT (a D3R-mediated behavior).WW-III-55 (10 mg/kg) inhibited the head twitch response (HTR) by 95% in DBA/2J mice.

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 Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.

Acetophenazine, a phenothiazine derivative, is an antipsychotic agent. Acetophenazine primarily blocks dopamine D2 receptors in the brain. Acetophenazine can be used for researching psychotic disorders such as schizophrenia and anxious depression.

Flupentixol is a high potency thioxanthene with D1 and D2 dopamine receptor antagonism. Flupentixol is used in therapy of schizophrenia as well as in anxiolytic and depressive disorders.

Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.

Razpipadon ((-)-PW0464), an aromatic compound, is a dopamine receptor partial agonist. Razpipadon can be used in the study of dopamine D1 ligand-mediated related psychiatric disorders.

Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia, cocaine addition, and obesity.

Ecopipam (SCH 39166) is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia, cocaine addition, and obesity.

Mosapramine (Clospipramine) is an orally active and potent dopamine receptor antagonist with high affinity to dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT2 receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research.

Thioproperazine (RP 7843) is an orally active antipsychotic agent with calming, antiemetic activity. Thioproperazine is effective in promoting the release of dopamine in rat striatum. Thioproperazine can be used in studies of schizophrenia and bipolar disorder.

(S)-Remoxipride ((-)-Remoxipride) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride can be used for the research of psychotic disorder.

L-745870 is a high-affinity, selective and orally active antagonist of human dopamine D4 receptor with Ki of 0.43 nM. L-745870 considerably weaker D2 and D3 receptors affinity with Ki of 960 nM and 2300 nM, respectively. L-745870 has excellent brain penetration.

PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research.

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.

UCM1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).

GSK598809 (GSK-598809) is a potent, selective dopamine D(3) receptor antagonist with Ki value of 6.2 nM, >100-fold selectivity over D2 receptor.