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Dopamine receptor agonists and antagonists act on the five G protein-coupled receptors that respond to dopamine. The receptors form two groups, with D1 and D5 in the D1-like class and D2, D3 and D4 in the D2-like class. D1-like receptors stimulate adenylyl cyclase, whereas D2-like receptors inhibit it and lower cyclic adenosine monophosphate (cAMP) levels. Dopamine signaling controls movement, reward, motivation and hormone release, and is studied in Parkinson's disease and psychiatric research. Ligands here include the agonist rotigotine HCl, the D2 antagonists L-741626 and domperidone, and the D3-preferring ligand BP897.
Synonyms: SB-277011A dihydrochloride; SB277011; SB 277011A
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0,
Synonyms: R 64 766 hydrochloride
Risperidone hydrochloride is a serotonin 5-HT2 receptor blocker and a potent dopamine D2 receptor antagonist, with Kis of 0.16, 1.4 nM for 5-HT2 and D2 receptor, respectively.
Synonyms: R 64 766 mesylate
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM).
Synonyms: JNJ37822681
JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.
Synonyms: DAN 2163 hydrochloride; DAN2163
Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
Synonyms: ACR16; ASP2314; FR310826
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist.
Synonyms: R-(+)-SCH-23390 maleate
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively.
SB-699551 free base is a selective antagonist of the 5-HT5A receptor, characterized by a pKi of 8.2 nM, which allows for effective brain penetration. It exhibits significant selectivity over various serotonin receptor subtypes, dopamine receptors, and the α1B adrenoceptor. This compound disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, influencing the phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. SB-699551 free base is valuable for research into anxiety, breast cancer, and Alzheimer's disease.
SB-699551 is a selective 5-HT5A receptor antagonist with a pKi of 8.2 nM, demonstrating significant brain penetrance. This compound exhibits high selectivity over various 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptors. By disrupting Gαi/o-coupled signaling and the PI3K/AKT/mTOR pathways, SB-699551 influences phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. It serves as a valuable tool in the study of anxiety, breast cancer, and Alzheimer's disease.
SNAP8719 free base is a selective antagonist of the α1D-adrenoceptor, exhibiting a pKi of 8.89. This compound also demonstrates affinity for dopamine D2 and 5-HT1A receptors, with pKi values of 5.98 and 6.47, respectively, while showing minimal interaction with the α2a-adrenoceptor. SNAP8719 free base is useful for investigating adrenergic signaling pathways and can potentiate twitch responses in physiological assays.
N-Desmethyl asenapine is a primary metabolite of Asenapine, an atypical antipsychotic agent. This compound functions as an antagonist at multiple receptor sites, including serotonin, adrenoceptors, dopamine receptors, and histamine receptors. N-Desmethyl asenapine is valuable for research into psychopharmacology and the pharmacokinetics of antipsychotic drugs. Its role in studying the therapeutic and side effects associated with Asenapine makes it a significant reagent in the field.
5-HT2A Antagonist 4 Methanesulfonate is a selective antagonist of both dopamine D2 receptors and serotonin 5HT2A receptors. This compound is primarily utilized in research concerning central nervous system disorders, facilitating the exploration of neuropharmacology and the modulation of neurotransmitter activity. Its dual receptor targeting makes it a valuable tool for studying the pathophysiology and treatment strategies for various neuropsychiatric conditions.
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Synonyms: HP 873 hydrochloride
Iloperidone hydrochloride is a dual D2 and 5-HT2 receptor antagonist. It is classified as an atypical antipsychotic and is primarily utilized in the treatment of schizophrenia symptoms. This compound is valuable for research focused on neuropharmacology and the elucidation of antipsychotic mechanisms.
1192U90 is an antipsychotic agent that acts primarily as a dopamine D2 receptor antagonist and a serotonin 5-HT1a receptor agonist. This compound is effective in reducing the spontaneous firing of neurons within the limbic dopamine system, highlighting its potential in the treatment of neuropsychiatric disorders. It serves as a valuable tool for research related to dopaminergic and serotonergic neurotransmission mechanisms.
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Abaperidone hydrochloride is a potent antagonist of the 5-HT2A receptor and dopamine D2 receptor, exhibiting IC50 values of 6.2 nM and 17 nM, respectively. This compound demonstrates significant affinity in modulating serotonergic and dopaminergic signaling pathways, making it a valuable tool for studying neuropharmacology and the treatment of psychiatric disorders. Research applications include investigations into schizophrenia, anxiety, and mood disorders.
RGH-1756 is a selective antagonist of the human D3 dopamine receptor, exhibiting pronounced effects in modulating dopaminergic pathways. This compound demonstrates lesser antagonistic activity on the human D2L and 5HT1A receptors. RGH-1756 is primarily utilized in research focusing on neuropharmacology and the mechanism of antipsychotic treatments, particularly in understanding conditions related to dopamine dysregulation.
Synonyms: CP-88059 mesylate
Ziprasidone mesylate is a potent antagonist of the 5-HT and dopamine receptors, specifically targeting the Rat D2 receptor (Ki=4.8 nM), the 5-HT2A receptor (Ki=0.42 nM), and the 5-HT1A receptor (Ki=3.4 nM). This compound demonstrates significant activity in modulating serotonergic and dopaminergic pathways, making it valuable for research in psychiatric disorders, such as schizophrenia and mood disorders. Its unique pharmacological profile allows for a better understanding of the interplay between these neurotransmitter systems in various biological contexts.
Synonyms: 3-Chlorocarpipramine dihydrochloride hydrate
Clocapramine dihydrochloride hydrate is a potent antagonist of the D2 and 5-HT2A receptors. It demonstrates significant biological activity by inhibiting the signaling pathways associated with these receptors, making it valuable for pharmacological research. This compound is particularly useful in studies related to neuropharmacology, psychopharmacology, and the development of therapeutic agents targeting psychiatric disorders.
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BGC20-761 is a selective antagonist of the 5-HT6 and dopamine receptors, exhibiting human receptor Ki values of 20 nM for 5-HT6, 69 nM for 5-HT2A, and 140 nM for D2. It has demonstrated the ability to enhance long-term memory, suggesting its potential utility in cognitive enhancement therapies. Additionally, BGC20-761 may serve as a promising candidate for the development of antipsychotic agents, supporting research in neuropharmacology and mental health disorders.
Synonyms: HF 1854 dihydrochloride
Clozapine dihydrochloride is an antipsychotic compound that primarily functions as a dopamine D2 receptor antagonist, exhibiting a Ki of 75 nM. It demonstrates significant affinity for muscarinic M1 and serotonin 5HT2A receptors, with Kis of 9.5 nM and 4 nM, respectively. Additionally, Clozapine acts as a potent and selective agonist at the muscarinic M4 receptor, with an EC50 of 11 nM. This compound is crucial for research into schizophrenia and related neuropsychiatric disorders.
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SB-773812 is a high-affinity antagonist of the serotonin 5-HT6 receptor, exhibiting a pKi of 8.1. Additionally, it demonstrates moderate to high affinity for dopamine receptors 2 and 3, with pKi values of 7.4 and 8.5, respectively. This compound is primarily used in research investigating central nervous system disorders, particularly those involving serotonin and dopamine signaling pathways. Its profile suggests potential applications in studying neuropharmacology and related therapeutic areas.
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Synonyms: Lu 31-130 fumarate
Zicronapine fumarate is a potent dopamine receptor antagonist primarily targeting D1 and D2 receptors, as well as serotonin 5-HT2A receptors. It exhibits significant pro-cognitive effects in preclinical models, positioning it as a promising candidate for the treatment of various neurological and psychiatric disorders. Research applications include the exploration of its therapeutic potential in conditions such as schizophrenia and mood disorders.
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Synonyms: Lu 31-130
Zicronapine is a potent dopamine receptor antagonist targeting both D1 and D2 subtypes, as well as serotonin receptor 5-HT2A. This compound demonstrates notable pro-cognitive effects in animal models, suggesting its potential utility in the treatment of various neurological and psychiatric disorders. Zicronapine's pharmacological profile makes it a valuable tool for research into psychotropic drug mechanisms and cognitive enhancement strategies.
Synonyms: (R)-Amisulpride hydrochloride; (R)-Esamisulpride hydrochloride; (R)-DAN 2163 hydrochloride
Aramisulpride hydrochloride is a potent 5-HT7 receptor antagonist with a Ki value of 22 nM, demonstrating significant affinity for the D2 and D3 dopamine receptors as well, with Ki values of 140 nM and 13.9 nM, respectively. This compound is primarily utilized in psychiatric research to investigate the roles of serotonin and dopamine pathways in mental health disorders. Its unique pharmacological profile makes it a valuable tool for exploring therapeutic interventions and understanding neurobiological mechanisms.
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Synonyms: LY 120363
Flumezapine is a potent antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine (5-HT) receptor. This compound has demonstrated the ability to inhibit conditioned avoidance responses in rodent models while maintaining a low risk of extrapyramidal side effects. Flumezapine is valuable in antipsychotic research, particularly in studies exploring the modulation of dopaminergic and serotonergic pathways without altering cortisol levels induced by κ-opioid receptor agonists.
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