Dopamine Receptors

Cat. No.

A29954

CAS No.

200398-40-9

S18327

S18327 is a selective antagonist of the D2 and 5-HT2A receptors, primarily targeting multiple neurotransmitter systems in the brain. Its pharmacological profile suggests efficacy in countering excessive dopamine activity and addressing glutamate hypo-function. S18327 has been shown to reproduce discriminative stimuli similar to Clozapine and may improve cognitive filtering deficits associated with schizophrenia while also exhibiting anxiolytic effects. Additionally, its reduced affinity for histaminergic and muscarinic receptors minimizes the risk of side effects commonly associated with other antipsychotic medications.

Cat. No.

A29956

CAS No.

1263278-77-8

4-Chloro Trazodone hydrochloride

4-Chloro Trazodone hydrochloride is a derivative of Trazodone hydrochloride, which functions primarily as a serotonin receptor antagonist and reuptake inhibitor. This compound exhibits key biological activity in the modulation of serotonergic activity, making it useful for investigating the mechanisms underlying anxiety disorders. It serves as a valuable tool in research applications focused on antipsychotic and antidepressant effects, contributing to the exploration of treatment options in mental health.

Cat. No.

A29974

CAS No.

132812-45-4

Blonanserin dihydrochloride

Synonyms: AD-5423 dihydrochloride

Blonanserin dihydrochloride is a potent antagonist of the 5-HT2A and dopamine D2 receptors, exhibiting Ki values of 0.812 nM and 0.142 nM, respectively. This compound is primarily utilized as an atypical antipsychotic agent and is relevant for research focused on extrapyramidal symptoms, sedation levels, and hypotensive effects. Its pharmacological profile makes it a valuable tool in the study of neuropsychiatric disorders and related therapeutic interventions.

Cat. No.

A30282

CAS No.

2413-38-9

Flupentixol dihydrochloride

Synonyms: Flupenthixol dihydrochloride

Flupentixol dihydrochloride is a potent antagonist of D1 and D2 dopamine receptors, demonstrating significant inhibition of PI3Kα with an IC50 of 127 nM. This compound exhibits anti-proliferative effects on cancer cells and promotes apoptosis, making it a valuable tool in oncology research. Additionally, Flupentixol has applications in studies related to schizophrenia, anxiety, and depression, contributing to the understanding of these complex neuropsychiatric disorders.

Cat. No.

A32141

CAS No.

156337-32-5

L 741742

L 741742 is a highly selective antagonist of the dopamine D4 receptor, exhibiting a Ki of 3.5 nM for this target and demonstrating significantly lower affinity for the D2 and D3 receptors. This compound effectively suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, disrupts lysosomal function, and impairs autophagic flux. L 741742 induces G0/G1 cell-cycle arrest and apoptosis, enhances neuronal differentiation in human neural stem cells, and selectively targets the growth of glioblastoma neural stem cells. Its potential therapeutic applications include research in schizophrenia and glioblastoma, with demonstrated synergy when combined with Temozolomide in vitro.

Cat. No.

A32393

CAS No.

2709-56-0

Flupentixol

Synonyms: Flupenthixol

Flupentixol is an orally active antagonist of D1 and D2 dopamine receptors. This compound exhibits anti-proliferative effects on cancer cells, promoting apoptosis, and has potential applications in the study of schizophrenia, anxiety, and depression. Additionally, Flupentixol has been identified as a new inhibitor of PI3Kα, with an IC50 value of 127 nM, making it a valuable reagent for research in neuropsychiatric disorders and cancer biology.

Cat. No.

A32672

CAS No.

2015-28-3

Perphenazine dihydrochloride

Perphenazine dihydrochloride is a potent antagonist of dopamine receptors, primarily targeting D2 and D3 subtypes, with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it exhibits activity against 5-HT2A and α1A adrenergic receptors. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis. Perphenazine dihydrochloride is particularly useful in research focused on mental disorders, oncology, and inflammatory processes.

Cat. No.

A32971

CAS No.

783334-36-1

Olanzapine hydrochloride

Synonyms: LY170053 hydrochloride

Olanzapine hydrochloride is a selective antagonist of serotonin receptors (5-HT2A/2C, 5-HT3) and dopamine receptors (D1, D2). It exhibits high affinity binding to various targets, including H1, muscarinic M1-5, and adrenergic α1 receptors, contributing to its pharmacological profile. This atypical antipsychotic is primarily used in research focusing on neuropharmacology, the treatment of schizophrenia, and mood disorders, providing valuable insights into the modulation of neurotransmitter systems.

Cat. No.

A33820

CAS No.

1420-55-9

Thiethylperazine

Thiethylperazine is a potent antagonist of dopamine D2 and histamine H1 receptors. This phenothiazine derivative exhibits notable anti-emetic, antipsychotic, and antimicrobial properties, making it valuable in various therapeutic contexts. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β (Aβ) load in murine models, thus highlighting its potential relevance in neurodegenerative research.

Cat. No.

A33878

CAS No.

1179-69-7

Thiethylperazine dimaleate

Thiethylperazine dimaleate is a phenothiazine derivative that functions as a potent antagonist of dopamine D2 and histamine H1 receptors. This compound demonstrates significant anti-emetic properties and has been shown to selectively activate ABCC1, leading to a reduction in amyloid-β (Aβ) load in murine models. Additionally, thiethylperazine dimaleate exhibits antipsychotic and antimicrobial activities, making it a valuable reagent for various biological research applications.

Cat. No.

A33916

CAS No.

314-03-4

Pimethixene

Synonyms: Pimetixene

Pimethixene is a potent antagonist of multiple receptor types, primarily functioning as a histamine receptor antagonist. It demonstrates significant activity against serotonin receptors (5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C), dopamine receptors (D2, D4), and muscarinic receptors (M1, M2), with reported pKis of 7.63 to 10.44. This pharmacological profile positions pimethixene as an effective agent for migraine management and offers valuable insights for research into antihistaminic and antiserotonergic therapies.

Cat. No.

A34022

CAS No.

5591-45-7

Thiothixene

Synonyms: NSC 108165; Navan; Navane

Thiothixene is a potent dopamine D2 receptor antagonist, exhibiting selectivity over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). This compound demonstrates significant biological activity by reducing spontaneous and amphetamine-induced locomotor activity in rodent models, thereby influencing behavioral paradigms. Additionally, thiothixene enhances latent inhibition and competitive behavior, suggesting potential applications in understanding psychotropic effects and selective attention. Its diverse receptor binding profile also includes interactions with serotonin, histamine, adrenergic, muscarinic acetylcholine, and sigma receptors, broadening its relevance in psychopharmacological research.

Cat. No.

A34075

CAS No.

1411867-74-7

Asenapine citrate

Synonyms: Org 5222 citrate

Asenapine citrate is a 5-HT receptor antagonist that exhibits potent activity against serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4), and histamine receptors (pKi: 8.2-9.0). This atypical antipsychotic compound is primarily utilized in research focusing on schizophrenia and bipolar disorder, helping to elucidate the mechanisms of these neuropsychiatric conditions.

Cat. No.

A34886

CAS No.

874882-93-6

L 741742 hydrochloride

L 741742 hydrochloride is a highly selective antagonist of the human D4 dopamine receptor, exhibiting a Ki value of 3.5 nM for the D4 receptor while demonstrating much lower affinity for D3 and D2 receptors. This compound disrupts signaling pathways associated with PDGFRβ, ERK1/2, and mTOR, and impairs autophagic processes by affecting lysosomal function. Biologically, it induces G0/G1 cell-cycle arrest and apoptosis in various cell types and promotes neuronal differentiation in human neural stem cells. L 741742 hydrochloride is particularly relevant for research on schizophrenia and glioblastoma, demonstrating efficacy against glioblastoma neural stem cells and enhancing the effects of Temozolomide in vitro.

Cat. No.

A39184

CAS No.

3082344-46-2

Dopamine D4 receptor ligand 3

Dopamine D4 receptor ligand 3 is a selective antagonist of the dopamine D4 receptor (D4R), exhibiting a pKi of 8.86. It demonstrates significant activity with pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 signaling pathways in HEK-293T cells, respectively. Additionally, this compound has been shown to inhibit cell viability in three human glioma cell lines—U87 MG, T98G, and U251 MG—while also inducing reactive oxygen species (ROS) production and mitochondrial dysfunction in these glioma cells. This makes it a valuable tool for studying the role of D4R antagonism in cancer biology and neuropharmacology.

Cat. No.

A39583

CAS No.

605-75-4

Trifluoperazine dimaleate

Trifluoperazine dimaleate is a potent dopamine receptor blocker, primarily indicated for research into antipsychotic mechanisms. This compound exhibits significant α1-adrenergic receptor antagonism and serves as an inhibitor of NUPR1, highlighting its potential anticancer properties. Additionally, trifluoperazine dimaleate functions as a calmodulin inhibitor and inhibits P-glycoprotein activity. Its versatile applications extend to studying schizophrenia and the reversible inhibition of influenza virus morphogenesis.

Cat. No.

A45811

CAS No.

5942-95-0

Carpipramine

Synonyms: Defekton

Carpipramine is an antipsychotic agent classified within the iminodibenzyl group, primarily functioning as a potent dopamine antagonist. It effectively blocks both alpha 1- and alpha 2-adrenoceptors, while also exhibiting antagonist properties at serotonin (5-HT2) receptors. Carpipramine demonstrates significant antipsychotic and antidepressant effects, making it valuable for research in neurological disorders, including post-traumatic stress disorder (PTSD) and depression.

Cat. No.

A45822

CAS No.

749-02-0

Spiperone

Synonyms: Spiroperidol

Spiperone is a potent antagonist of dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A receptors. With its capability to enhance intracellular calcium levels and inhibit the Wnt signaling pathway, Spiperone serves as a valuable tool in the study of neurological disorders. Its role as a labeled ligand for neuroleptic receptors further underscores its utility in receptor binding studies and neurotransmitter research. This compound is particularly relevant for investigating the mechanisms underlying various neuropsychiatric conditions.

Cat. No.

A45832

CAS No.

99295-33-7

SKF-83566

SKF-83566 is a selective antagonist of the D1-like dopamine receptors, specifically targeting the dopamine D1 and D5 receptors. This compound exhibits potent inhibition of the dopamine transporter (DAT) with an IC50 of 5.7 μM, and shows competitive antagonism at the vascular 5-HT2 receptor. In addition, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it relevant for research into neurological disorders such as Parkinson's disease and studies focused on alleviating nicotine cravings.

Cat. No.

A45833

CAS No.

190133-94-9

Ecopipam hydrochloride

Synonyms: SCH 39166 hydrochloride

Ecopipam hydrochloride is a potent and selective antagonist of the dopamine D1 and D5 receptors, with inhibition constants (Ki) of 1.2 nM and 2.0 nM, respectively. This compound demonstrates over 40-fold selectivity against D2, D4, 5-HT, and α2a receptors, with Ki values of 0.98 μM, 5.52 μM, 0.08 μM, and 0.73 μM, respectively. Ecopipam hydrochloride is applicable in research focused on schizophrenia and obesity, providing a valuable tool for studying these conditions.

Cat. No.

A45850

CAS No.

215804-67-4

SB-277011 hydrochloride

Synonyms: SB-277011A hydrochloride

SB-277011 hydrochloride is a selective antagonist of the dopamine D3 receptor (D3R), demonstrating potent inhibition with Ki values of 10.7 nM in rodents and 11.2 nM in humans. This compound exhibits significant selectivity, with an 80- to 100-fold preference for D3R over other dopamine receptors, including D2, 5-HT1B, and 5-HT1D. Due to its ability to penetrate the brain and oral bioavailability, SB-277011 hydrochloride is valuable in research investigating the role of D3R in various neurological and psychiatric disorders.

Cat. No.

A45851

CAS No.

199739-10-1

Paliperidone palmitate

Synonyms: 9-Hydroxyrisperidone palmitate

Paliperidone palmitate is a competitive antagonist of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A) receptors with the capability to cross the blood-brain barrier. By binding to these receptors, it modulates the activity of dopamine and serotonin, thereby exerting antipsychotic effects. This compound is primarily utilized in research related to schizophrenia and other neuropsychiatric disorders, contributing to the understanding of antipsychotic mechanisms and therapeutic strategies.

Cat. No.

A45859

CAS No.

478-84-2

2-Bromo-LSD

Synonyms: BOL-148; Bromolysergide

2-Bromo-LSD (BOL-148; Bromolysergide) is a potent dopamine receptor antagonist specifically targeting dopamine neurons in the substantia nigra and neostriatum. It enhances the hydroxylation of tyrosine within the striatum and mitigates the reduction of Apomorphine-induced DOPA accumulation. Additionally, 2-Bromo-LSD inhibits 5-HT receptor-mediated DOPA formation, making it valuable for research on neurotransmitter regulation and potential therapeutic applications in neuropharmacology.

Cat. No.

A45873

CAS No.

2022-29-9

Spiperone hydrochloride

Synonyms: Spiroperidol hydrochloride

Spiperone hydrochloride is a potent antagonist of dopamine D2 and 5-HT2A receptors, exhibiting Ki values of 0.06 nM and 1 nM, respectively. In addition, it selectively antagonizes the α1B-adrenoceptor and activates calcium-activated chloride channels (CaCC). This compound has demonstrated significant antipsychotic and anti-inflammatory properties, making it a valuable tool for research in neuropharmacology and inflammation studies.

Cat. No.

A45906

CAS No.

75272-39-8

Nemonapride

Synonyms: YM-09151-2; Emonapride

Nemonapride is a highly potent antagonist of the dopamine D2 receptor, exhibiting a Ki of 0.06 nM. Additionally, it activates the 5-HT1A receptor with an IC50 of 34 nM. This compound functions as an antipsychotic and efficiently crosses the blood-brain barrier, demonstrating significant neuroleptic effects in animal models. It is valuable for research focused on neuropharmacology and the mechanisms underlying psychiatric disorders.