D₄ Receptor Antagonist

Raclopride is a dopamine D₂/D₃ receptor antagonist with potential antipsychotic effects. Raclopride binds to D₂ and D₃ receptors with K_is of 1.8 nM and 3.5 nM, respectively.

NRA‑0562 is a dopamine antagonist with high affinities for dopamine D₁/D₂/D₃/D₄, 5‑HT₂A and α₁‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED₅₀ = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia..

Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.

L-741626 is a selective D2 dopamine receptor antagonist, with the K_i values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively.

Blonanserin (AD-5423) is a potent and orally active 5-HT_2A (K_i=0.812 nM) and dopamine D2 receptor (K_i =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with K_is 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 (K_i=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity.

L-745870 is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

Iloperidone (HP 873) is a D₂/5-HT₂ receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.

Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.

L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D₂ receptor (K_i values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors, respectively) and 5-HT_2A/5-HT_1A receptor (K_is of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities.

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

Pipamperone (Floropipamide) is a butyrophenone derivative and high-affinity antagonist of 5-HT_2A receptor (pK_i=8.2) and D₄ receptor (pK_i=8.0). Pipamperone is also a low-affinity antagonist of D₂ receptor (pK_i=6.7). Pipamperone affects neurotransmitter functions and exerts antipsychotic activity. Pipamperone is used in the research of mental disorders such as autism-related behavioral disorders and Alzheimer's disease.

Dopamine D4 receptor antagonist-1 is a selective DRD4 antagonists, with a K_i of 9.0 nM for Hd4.2. Dopamine D4 receptor antagonist-1 can be used in study of schizophrenia.

Sonepiprazole (PNU-101387G) is a selective D4 dopamine antagonist with K_is of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively.

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

L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with K_i values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma.

NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (K_i = 3.6 nM). NGD94-1 modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD94-1 can be used for neurological disease research^[1][2].

Adoprazine (SLV313) is a full 5-HT_1A receptor agonist with a pEC₅₀ of 9 at cloned h5-HT_1A receptors. Adoprazine (SLV313) is a full D₂ and D₃ receptor antagonist with pA₂s of 9.3 and 8.9 at hD₂ and hD₃ receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics.

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