D₂ Receptor Antagonist

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.

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.

Chlorprothixene is a dopamine and histamine receptors antagonist with K_is of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.

Promazine (Romtiazin) hydrochloride is an antipsychotic and a dopamine receptor D₂ antagonist. Promazine hydrochloride inhibits dopaminergic neurotransmission.

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

Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects.

Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with K_is of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor (D₃R) antagonist with K_i values of 10.7 nM and 11.2 nM at rodent and human D₃R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pK_is of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT_1B, and 5-HT_1D receptors, respectively.

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.

Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis. Pericyazine is a selective D2-dopamine receptor antagonist. Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects.

Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia.

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.

Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate 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).

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.

Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [³⁵S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.

Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic agent. Haloperidol hydrochloride can be used in the study of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.

Metoclopramide hydrochloride hydrate is a potent antagonist of 5-HT₃ and dopamine D2 receptor, with IC₅₀s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride hydrate can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.

Ziprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride 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).

Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT₂ and dopamine D₂ antagonist, and a 5-HT_1A agonist, with K_is of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT₂, a₁-adrenergic receptor, dopamine D₂, histamine H₁ and a₂-adrenergic receptor, respectively, and a pEC₅₀ and pK_i of 7.60 and 8.08 for h5-HT_1A.