D₂ Receptor Antagonist

Ordopidine is a dopamine D2 receptor antagonist. Ordopidine can inhibit hyperactivity caused by psychostimulants. Ordopidine can be used in neurological research.

EF-7412 is a dual antagonist of the 5-HT₁A receptor and dopamine D₂ receptor, with K_i values of 27 nM and 22 nM, respectively. EF-7412 acts as an antagonist at both pre- and postsynaptic 5-HT₁A receptor sites, blocking 8-OH-DPAT (HY-112061)-induced hypothermia, behavioral syndrome, and corticosterone elevation in vivo. EF-7412 increases hypothalamic 5-HIAA/5-HT and DOPAC/DA ratios, alters 5-HT and DA neuronal activity, and slightly decreases spontaneous motor activity. EF-7412 can be used for research on 5-HT₁A/D₂ receptor regulation and related neural pathways.

BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC₅₀s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC₅₀s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.

Dehydrohaloperidol, Haloperidol (HY-14538) analogue, is a selective human dopamine D₂ receptor antagonist with a pK_d of 8 and a pk_i of 8. Dehydrohaloperidol can be used for the research of schizophrenia.

Asenapine citrate, 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 citrate can be used in the research of schizophrenia and bipolar disorder.

Flupentixol is an orally active D₁/D₂ dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC₅₀=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.

SB-773812 is a moderate-affinity antagonist at dopamine receptor 2 (pKi=7.4) and a high-affinity antagonist at the dopamine receptor 3 (pKi=8.5) and at the serotonin 5-hydroxytryptamine receptors 2A (pKi=9.0), 2C (pKi=8.1), and 6 (pKi=8.1). SB-773812 is promising for research of central nervous system disorders.

SSR-181507 hydrochloride is a dopamine D₂ receptor antagonist and 5-HT_1A receptor agonist. SSR-181507 antagonizes Apomorphine (HY-12723)-induced climbing in mice and stereotypies in rats. SSR-181507 hydrochloride can be used in the research of depression and anxiety.

SB-414796 is a selective, orally active and cross the blood-brain barrier dopamine D3 receptor antagonist with K_i values of 4, 400 nM for D3, D2, respectively.

Flupenthixol decanoate is a dopamine D2 receptor antagonist with antipsychotic effects. Flupenthixol decanoate can be used for schizophrenia and depression research.

Clocapramine hydrochloride hydrate is an antagonist of the D₂ and 5-HT_2A receptors.

BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor K_i values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent.

PF-4363467, a dopamine D3/D2 receptor antagonist, attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-4363467 exhibits K_i values of 3.1 nM and 692 nM for D3R and D2R.

Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

Haloperidol-¹³C₆ is the ¹³C₆ labeled Haloperidol. Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.

Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT_1A, 5-HT_2A, 5-HT_2C, D₂ and H₁ receptors with K_is of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability.

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 K_i values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research.

Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

A-69024 is a selectivity dopamine D-1 receptor antagonist with the K_i values of 12.6 nM and 1290 nM for dopamine D-1 receptor and dopamine D-2 receptor, respectively.

Perphenazine dihydrochloride 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 dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation.