Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].
Bulbocapnine hydrochloride, an aporphine alkaloid, is a dopamine receptor inhibitor. Bulbocapnine hydrochloride inhibits dopamine synthesis. Bulbocapnine hydrochloride also has neuroleptic-like, anticonvulsant and antinociceptive effects[1][2][3].
Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.
A-437203 is a selective D3 receptor antagonist with Ki of 71, 1.6, and 6220 nM for D2, D3, and D4 receptors, respectively.
LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay[1][2].
L-745870 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 has excellent brain penetration[1][2][3].
ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].
(R)-SKF 38393 ((±)-SKF-38393) hydrochloride is a potent and selective D1 dopamine receptor antagonist. (R)-SKF 38393 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channel[1].
NGB 2904 is an orally active and selective dopamine (DA) D3 receptor antagonist. NGB 2904 can be used for the research of cocaine addiction[1].
PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis[1][2].
Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].
A68930, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis[1].
Acetophenazine, a phenothiazine derivative, is an antipsychotic agent. Acetophenazine primarily blocks dopamine D2 receptors in the brain. Acetophenazine can be used for researching psychotic disorders such as schizophrenia and anxious depression[1][2].
Brexpiprazole (OPC-34712) hydrochloride, 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 hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[1][2].
Pramipexole 2Hcl is a partial/full D2S, D2L, D3, D4 receptor agonist with a Ki of 3.9, 2.2, 0.5 and 5.1 nM for D2S, D2L, D3, D4 receptor, respectively. IC50 Value: 3.9 nM(D2S); 2.2 nM(D2L); 0.5 nM(D3); 5.1 nM(D4)Target: Dopamine ReceptorPramipexole dihydrochloride is a dopamine receptor agonist with selectivity for the D3 receptor (Ki values are 3.9, 3.3, 0.5 and 3.9 nM for D2L, D2S, D3 and D4 receptors respectively). Pramipexole dihydrochloride exhibits negligable affinity for D1 and D5 receptors. Pramipexole has been found to have neuroprotective effects independent of its dopamine receptor agonism. It reduces mitochondrial reactive oxygen species (ROS) production and inhibits the activation of apoptotic pathways. Pramipexole displays activity in the treatment of Parkinson's disease (PD) and restless legs syndrome (RLS).
Haloperidol D4' is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.
Fluphenazine decanoate is a long-acting phenothiazine neuroleptic that used to treat schizophrenia. Fluphenazine decanoate is also a high and continuous dopamine D2 receptor blocker[1][2][3].
Chlorpromazine Hydrochloride is an antagonist of the dopamine D2, 5HT2A, potassium channel andsodium channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.
YQA14 is a selective antagonist of D3 receptor.
rac-Rotigotine Hcl is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM. IC50 Value: 0.69 nM(Ki)Target: D-2 receptorin vitro: rac-Rotigotine showed high potency (Ki = 0.69 nM) and selectivity for D-2 receptors as compared to its potency and selectivity at various other neuronal receptors (Ki in nM): D-1 (678) dopamine, alpha 1-(534) and alpha 2-(195) adrenoceptor, S1-(6940) and S2-(5900) serotonin and muscarine (2660). Very low activity (Ki greater than 10(-5) M) was seen at the beta-adrenoceptor, A1-adenosine, GABAA and benzodiazepine receptors. Furthermore, rac-Rotigotine inhibited the calcium-dependent release of [3H]dopamine (IC50: 4 nM) and [3H]acetylcholine (IC50: 6.3 nM) from rabbit striatal slices in the nanomolar range. These effects of rac-Rotigotine were mediated through activation of D-2 dopamine autoreceptors and D-2 dopamine heteroreceptors, respectively.in vivo: Presynaptic dopaminergic activity in vivo was measurable as an inhibition of the locomotor activity of mice, and in this model rac-Rotigotine was more effective than apomorphine. Moreover, the effect of rac-Rotigotine could be antagonized by sulpiride but not by yohimbine. rac-Rotigotine was equipotent with apomorphine in inducing circling behaviour in 6-OHDA-lesioned rats. rac-Rotigotine had almost no serotonergic activity in vivo.
NGD94-1 is a specific dopamine D4 receptor antagonist. NGD94-1 can effectively reverse Phencyclidine-induced cognitive impairment in marmosets. NGD94-1 can be used in the study of psychiatric diseases[1].
Talipexole (B-HT920) is a dopamine agonist that has been proposed as an antiparkinsonian agent.Target: Dopamine ReceptorB-HT920 is a selective alpha 2-adrenoceptor agonist. The effects of B-HT920 have been specified using the alpha-adrenergic antagonists yohimbine and prazosin and the dopamine antagonist haloperidol. Yohimbine could not antagonize any of the actions of B-HT920. Pretreatment with prazosin showed a decrease in the loss of body weight caused by B-HT920, while pretreatment with yohimbine showed that B-HT920 induced an increased loss in body weight. These data suggest that B-HT920 under certain conditions exerts dopamine-agonistic actions in stimulating locomotor activity and alpha 1-adrenergic actions in inducing salivation and enhanced loss of body weight [1]. Concomitant treatment with talipexole, an anti-parkinsonian drug, inhibited MPTP-induced autolysis and individual death in a concentration-dependent manner. Pramipexole showed a similar protective effect. In addition, post-treatment with talipexole at 1 hr after MPTP completely inhibited MPTP-induced individual death. Although MPTP treatment caused 30% of the planarians to undergo autolysis and individual death within 12 hr, post-treatment with talipexole even at 12 hr completely rescued the remaining 70% of the planarians from death. These results suggest that the MPTP-treated planarian may be useful as a novel parkinsonian model in which talipexole has a protective effect even in the case of post-treatment [2].
Dexpramipexole 2Hcl(KNS-760704), also known as R-(+)-Pramipexole, is a neuroprotective agent and weak non-ergoline dopamine agonist. IC50 Value:Target: Dopamine ReceptorDexpramipexole has been found to have neuroprotective effects and is being investigated for treatment of amyotrophic lateral sclerosis (ALS). Dexpramipexole reduces mitochondrial reactive oxygen species (ROS) production, inhibits the activation of apoptotic pathways, and increase cell survival in response to a variety of neurotoxins and β-amyloid neurotoxicity. Compared to the S-(-) isomer, Dexpramipexole has much lower dopamine agonist activity.
Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. 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][3].
Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].
RMI-61140 is an orally active neuroleptics. RMI-61140 decreases spontaneous motility and muscle tone in mice. RMI-61140 increases barbit urate-induced sleep and causes eyelid ptosis. RMI-61140 can be used for schizophrenia research[1].
Trazpiroben (TAK-906) is a dopamine D2/D3 receptor antagonist used for chronic research of moderate-to-severe gastroparesis[1].
NMI 8739 is a dopamine D2 autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.
Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).