dopaminereceptor

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

Pentiapine (CGS 10746) is a novel inhibitor of dopamine release.

ONC206, an analogue of the TRAIL inducer ONC201, acts as a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations and possesses broad-spectrum anti-tumor activity.

MPTP hydrochloride is a dopamine neurotoxin and the precursor of MPP⁺. It can induce apoptosis and has the ability to cross the blood-brain barrier. MPTP hydrochloride is toxic to dopaminergic neurons and is commonly used for the construction of Parkinson's disease animal models.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ff old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.

(Rac)-AMXT-1501 4HCl is a polyamine transport inhibitor that inhibits polyamine transport and acts synergistically with cisplatin in HNSCC. (Rac)-AMXT-1501 4HCl has potential antimicrobial activity and inhibits neuroblastoma cell proliferation and pneumococcal pod biosynthesis by targeting ornithine decarboxylase and polyamine transport.

Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective dopamine D2 receptor agonist with in vivo antihypertensive activity.

NMI 8739 (n-docosahexaenoyl dopamine) is an agonist of D2 autoreceptor. NMI 8739 reduces NO production and elicits concentration-dependent suppression of CCL-20, MCP-1 and IL-6 release.

JNJ-37822681 has potential for the treatment of schizophrenia and bipolar disorder.JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2

PD 168568 dihydrochloride (PD 168568 (dihydrochloride)) is an orally active and selective antagonist of D4 dopamine receptor(Ki of 8.8 nM).

PNU-177864 hydrochloride is a potent, selective, and orally active dopamine D3 receptor antagonist that is structurally consistent with a cationic amphiphilic drug (CAD). It induces phospholipidosis in vivo and exhibits antischizophrenic activity.

SB-277011 (SB-277011A) is a specific antagonist of the dopamine D3 receptor with pKi values of 8.0, 6.0, 5.0, and <5.2 for D3 receptor, D2 receptor, 5-HT1D, and 5-HT1B respectively.

Tedatioxetine hydrobromide (Lu AA 24530 hydrobromide) is a serotonin-norepinephrine-dopamine reuptake inhibitor and an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors, which can be used to treat depression and anxiety.

SPD-473 citrate (BTS 74398 citrate) is a dopamine reuptake inhibitor, a norepinephrine transporter protein (NET) inhibitor, and a 5-hydroxytryptamine reuptake inhibitor, and is used in the study of neurological disorders and endocrine and metabolic diseases.

Abaperidone is a potent 5-HT2A receptor and dopamine D2 receptor antagonist with an IC50 of 6.2 for 5-HT2A receptors and 17 nM for dopamine D2 receptors.Abaperidone is a potentially atypical anti-psychotropic compound that reduces basal hsp70 mRNA expression in rat striatum and prefrontal cortex. expression in the striatum and prefrontal cortex of rats.

Didesmethyl cariprazine, a metabolite of Cariprazine, is the major cyclic active part. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a potent D3 preference D3/D2 receptor partial agonist of dopamine for the treatment of schizophrenia, bipolar mania, and depression, with a high affinity for d3 and d2 receptors and a moderate affinity for 5-HT 1A receptors.

Halopemide is a potent inhibitor of PLD (IC50 = 220 and 310 nM for human PLD1 and PLD2). Halopemid is an antagonist of dopamine receptors. Halopemid can be used in psychotropic research.

Molindone ((±)-Molindone) is a therapeutic antipsychotic used to treat schizophrenia by blocking the action of dopamine in the brain. molindone is often used in combination with serotonin in a dose-dependent manner to increase errors and decrease response rates.

A 77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM). A 77636 hydrochloride shows antiparkinsonian activity. A 77636 hydrochloride is functionally inactive at dopamine D2 receptor.

6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for presynaptic melatonin receptor sites in the rabbit retina, inhibiting the calcium-dependent release of [3H]dopamine with higher metabolic stability than melatonin. Chloromelatonin competitively binds to [3H]melatonin at MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.

dopamine D1 receptor antagonist

NGD 94-1 is a selective D4 receptor antagonist with an affinity of 3 nM for the D4 receptor and greater than 2 pM for the D1, D2, D3, and D5 receptors.NGD 94-1 can be used in the study of cognitive disorders and other psychiatric disorders.

PAOPA is a novel dopamine D2 receptor modulator and L-proline-L-leucine-glycine amide (PLG) peptide mimetic that prevents and reverses behavioral and biochemical abnormalities in preclinical animal models of schizophrenia sensitized to amphetamine. PAOPA has been used in the study of schizophrenia and extrapyramidal dysfunction.