Highly selective D2 dopamine receptor antagonist
Ziprasidone(CP88059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.IC50 value:Target: 5-HT receptor; Dopamine receptorZiprasidone possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. Ziprasidone also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential [1]. Ziprasidone sulfoxide and sulfone were the major metabolites in human serum. The affinities of the sulfoxide and sulfone metabolites for 5-HT2 and D2 receptors are low with respect to ziprasidone, and are thus unlikely to contribute to its antipsychotic effects [2]. Ziprasidone was associated with significant differential adverse effects relative to placebo in BPM, BPD, and schizophrenia with no significant difference in weight gain in all 3 groups. Self-reported somnolence was increased across the 3 conditions. Subjects with BPM were more vulnerable to EPS than those with BPD or schizophrenia [3].Clinical indications: Bipolar I disorder; Bipolar disorder; Mania; SchizophreniaFDA Approved Date: February 2001
Quinpirole (Hydrochloride) is a high-affinity agonist dopamine D2/D3 receptor.
Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases[1][2][3].
Quetiapine Sulfoxide is a metabolite of Quetiapine. Quetiapine is an atypical antipsychotic approved for the treatment of schizophrenia, bipolar disorder, and along with an antidepressant to treat major depressive disorder.
Quetiapine D4 hemifumarate is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects[1].
Clozapine N-oxide (CNO) is a major metabolite of the anti-psychotic drug clozapine. Clozapine N-oxide is a agonist for the chemogenetic Designer Receptors Exclusively Activated by Designer Drug (DREADD) system.
Tetrahydropalmatine, an active component isolated from corydalis, acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
Olanzapine D3 (LY170053 D3) is the deuterium labeled Olanzapine. Olanzapine is 5-HT2 and D1/D2 antagonist. Olanzapine is an antipsychotic agent with anticholinergic properties[1]. Olanzapine induces autophagy, mitochondrial damage and mitophagy in human SH-SY5Y neuronal cell line[2].
Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class.
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively[1].
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects of morphine and stress-induced analgesia (SIA). MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB)[1][2][3].
Sulpiride is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class, used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression.
Dopamine D4 receptor antagonist-1 is a selective DRD4 antagonists, with a Ki of 9.0 nM for Hd4.2. Dopamine D4 receptor antagonist-1 can be used in study of schizophrenia[1].
Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).
Fluphenazine dihydrochloride is a phenothiazine-class D1DR and D2DR inhibitor; used to deliver Fluphenazine to biological systems in studies probing the effects and metabolic fates of this commonly used dopamine antagonist.
A68930 hydrochloride, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis[1].
Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
Benztropine mesylate is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research[1]. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2].
N-Despropyl Ropinirole (SKF-104557) is an active metabolite of the dopamine D2 receptor agonist Ropinirole (HY-B0623). N-Despropyl Ropinirole is a full agonist at human D2 and D3 receptors. N-Despropyl Ropinirole is a partial agonistof the hD4 receptor[1].
Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities[1][2][3].
Flupentixol is a high potency thioxanthene with D1 and D2 dopamine receptor antagonism. Flupentixol is used in therapy of schizophrenia as well as in anxiolytic and depressive disorders[1][2].
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions[1].
Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension[1][2].
Alizapride is a potent antiemetic, acting as a dopamine receptor antagonist. Alizapride also used in human digestive disorders[1][3].
L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors affinity. L-745870 hydrochloride has excellent brain penetration[1][2][3].
Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity. Cyclo(glycyl-L-leucyl) inhibits the development of Morphine induced pain relief as well as dopamine receptor supersensitivity in rats. Cyclo(glycyl-L-leucyl) has the potential for the prevention of tardive and/or L-DOPA (HY-N0304)-induced dyskinesias[1][2].
Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD)[1][2].
Tiapride, an atypical neuroleptic agent, is a selective dopamine D2-receptor antagonist with little propensity for causing catalepsy and sedation. The IC50 values of Tiapride are 1440, 45.8, >100, and 11.7 μM for D1; D2; D3; D4, respectively[1].
SKF 82958 hydrobromide is a D1/D5 receptor full agonist. IC50 value:Target: D1/D5 receptorin vitro: Neuropeptide and immediate early gene expression in striatonigral neurons of the normosensitive striatum is induced by mixed D1 receptor SKF-82958, which induces behavioral activity and preprodynorphin (PPD) and substance P (SP) gene expression in medium spiny neurons in the dorsal, and especially, in the ventral striatum. in vivo:Quantitative in situ hybridization was used to examine the contribution of muscarinic receptors to the transynaptic regulation of striatal gene expression induced by D1receptor activation. The acute injection of the full D1 agonist, SKF-82958, would induce PPD, SP and PPE mRNA expression in the intact rat striatum.