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].
SCH 23390 hydrochloride is a potent dopamine receptor D1 antagonist with Ki values of 0.2 and 0.3 nM for the D1 and D5.
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].
CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity[1].
FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease[1][2].
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride specifically activates the DREADD receptor hM3Dq. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier[1][2][3]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[4][5].
SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors[1].
BP 897 is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors, and shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 µM, respectively).
Pericyazine-d4 (Propericiazine-d4) is the deuterium labeled Pericyazine. 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[1]. Pericyazine is a selective D2-dopamine receptor antagonist[2][3]. Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects[4].
Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia[1][2].
Ropinirole-d3 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
SKF 81297 is a potent and selective dopamine D1 receptor agonist[1].
GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.IC50 value: 9.4/8.5/9.7 (pKi) [1]Target: 5-HT in vitro: GSK163090 demonstrates clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg. GSK163090 was devoid of agonist activity at R1 receptors, but rather it demonstrated amoderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9). [1]in vivo: Fromamong these analogues, the cyclic urea derivative, GSK163090, emerged due to its low hERG affinity and excellent in vitro DMPK profile. The superior quality of GSK163090 was further highlighted by its commendable in vivo pharmacokineticprofile in rat and its outstanding activity in the 5-HT1A PD model, where 50% efficacy was achieved at a blood concentration of 3 ng/mL. On the basis of these results and its promising preclinical developability profile, GSK163090 was selected as an appropriate development candidate for progression toward clinical proof-of-concept studies. [1]
Pentiapine is a novel dopamine release inhibitor.
PNU-96415E is a selective D4/5-HT2A antagonist. PNU-96415E may have potential antipsychotic efficacy[1].
L-DOPA-13C is the 13C labeled L-DOPA[1]. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[2][3][4].
SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression[1][2][3][4].
Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
Dexpramipexole-d3 ((R)-Pramipexole-d3) dihydrochloride is the deuterium labeled Dexpramipexole. Dexpramipexole((R)-Pramipexole), also known as R-(+)-Pramipexole, is a neuroprotective agent and weak non-ergoline dopamine agonist[1][2].
Sultopride hydrochloride is a selective antagonist of dopamine D2 receptor.
Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.
Dopamine HCl is a catecholamine neurotransmitter present in a wide variety of animals,And a dopamine D1-5 receptors agonist.Target: Dopamine ReceptorDopamine (or 3,4-dihydroxyphenethylamine) is a neuroendocrine transmitter in the catecholamine and phenethylamine families that plays a number of important roles in the brain and bodies of humans. Several important diseases of the nervous system are associated with dysfunctions of the dopamine system. Outside the nervous system, dopamine functions in several parts of the body as a local chemical messenger. In the blood vessels, it inhibits norepinephrine release and acts as a vasodilator; in the kidneys, it increases sodium excretion and urine output; in the pancreas, it reduces insulin production; in the digestive system, it reduces gastrointestinal motility and protects intestinal mucosa; and in the immune system, it reduces the activity of lymphocytes. A variety of important drugs work by altering the way the body makes or uses dopamine. Dopamine itself is available for intravenous injection: although it cannot reach the brain from the bloodstream, its peripheral effects make it useful in the treatment of heart failure or shock, especially in newborn babies. L-DOPA, the metabolic precursor of dopamine, does reach the brain and is the most widely used treatment for Parkinson's disease. From Wikipedia.
cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with Ki values of 0.38 nM and 7 nM for D2 receptor and 5-HT2A, respectively[1][2].
L-Stepholidine (Stepholidine), an alkaloid extract of the Chinese herb Stephania intermedia, is the first compound known to exhibit mixed dopamine D1 receptor agonist/D2 antagonist properties. L-Stepholidine (Stepholidine) has neuroprotective effect and inhibits heroin-induced reinstatement. L-Stepholidine (Stepholidine) is a potential medication for the treatment of opiate addiction[1][2][3].
ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons[1].
N-Methyldopamine hydrochloride is a precursor of adrenaline in the adrenal medulla. N-Methyldopamine hydrochloride is a modification of the dopamine (DA), and retains agonist activity at the DA1 receptor. N-Methyldopamine hydrochloride remains capable of universal surface coating and secondary reactions using the surface catechols. N-Methyldopamine hydrochloride can be used for heart failure research[1][2][3].
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19[1][2][3][4].
Sultopride is a selective antagonist of dopamine D2 receptor.