3-O-Methyldopa D3 (3-Methoxy-L-tyrosine D3) is deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
Quetiapine fumarate is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.IC50 value: Target: 5-HT ReceptorQuetiapine is indicated for the treatment of schizophrenia as well as for the treatment of acute manic episodes associated with bipolar I disorder. The antipsychotic effect of quetiapine is thought by some to be mediated through antagonist activity at dopamine and serotonin receptors. Specifically the D1 and D2 dopamine, the alpha 1 adrenoreceptor and alpha 2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also has an antagonistic effect on the histamine H1 receptor.
Mesdopetam (IRL790) is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam is used for the research of motor and psychiatric complications in Parkinson disease[1][2].
Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.IC50 value: 8.1/8.6/8.5 (pKi, for D2/ D3/5-HT1A receptor)Target: dopamine D2 and D3 receptor, 5-HT1A receptorin vitro: Pardoprunox also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity. Pardoprunox acts as a potent but partial D(2) receptor agonist (pEC50 = 8.0 and pA2 = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox acts as a partial agonist in the induction of [35S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [35S]GTPgammaS binding (pA2 = 9.0). Pardoprunox acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50 = 6.3) [1].in vivo: Pardoprunox induces contralateral turning behaviour in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra pars compacta (SNpc) (MED=0.03mg/kg; po). In MPTP-treated common marmosets, Pardoprunox dose-dependently increases locomotor activity (MED=0.03mg/kg; po) and decreases motor disability (MED=0.03mg/kg; po). In contrast Pardoprunox attenuated novelty-induced locomotor activity (MED=0.01mg/kg; po), (+)-amphetamine-induced hyperlocomotion (MED=0.3mg/kg; po) and apomorphine-induced climbing (MED=0.6mg/kg; po) in rodents. Pardoprunox also induces 5-HT1A receptor-mediated behaviours, including flat body posture and lower lip retraction (MED=0.3mg/kg; po). Collectively, these findings demonstrate that Pardoprunox possesses dopamine D2/3 partial agonist effects, 5-HT1A agonist effects and reduces parkinsonism in animal models. functional D2 receptor partial agonist activity and is effective in experimental models predictive of efficacy in PD.[2]
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7)[1].
(+)-Dihydrexidine hydrochloride is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM.
Razpipadon ((-)-PW0464), an aromatic compound, is a dopamine receptor partial agonist. Razpipadon can be used in the study of dopamine D1 ligand-mediated related psychiatric disorders[1][2].
SCH 39166 hydrobromide (SCH391660) is potent and selective antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. SCH 39166 hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). SCH 39166 hydrobromide can be used for the research of schizophrenia, cocaine addition, and obesity[1].
Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18. Benzamide Derivative 1 may be useful in treatment of gastrointestinal disorders.
Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Org-10490 is an antagonist of dopamine D1 receptor and dopamine D2 receptor, used for the treatment for psychiatric disease.
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.
Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%); also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity.IC50 value:Target:in vitro: SLV308 acted as a potent but partial D(2) receptor agonist (pEC(50) = 8.0 and pA(2) = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D(3) receptors, SLV308 acted as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA(2) = 9.0). SLV308 acted as a full 5-HT(1) (A) receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT(1) (A) receptors but with low potency (pEC(50) = 6.3) [1].in vivo: Unified PD Rating Scale (UPDRS)-Motor score was improved in pardoprunox-treated patients (overall mean dose 23.8 mg/d; -7.3 points), as compared with placebo (-3.0 points; P = 0.0001), from baseline to end point. At end point, there were more responders (> or = 30% reduction in UPDRS-Motor score) in the pardoprunox group (50.7%) than in the placebo group (15.7%; P < 0.0001) [2]. Surprisingly in the SNc, pardoprunox (10 μg kg?1, i.v.) either partially or fully suppressed the firing activity in two separate populations of DA neurons. Finally, in the DRN, pardoprunox (5-40 μg kg-1, i.v.) completely suppressed the firing activity of 5-HT neurons. Moreover, the selective 5-HT(1A) receptor antagonist WAY-100,635 prevented and reversed the effects of pardoprunox [3].
B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.IC50 Value: 25 nM(Adrenergic receptor α-2, rat)Target: Adrenergic Receptor; 5-HT Receptor; Dopamine Receptorin vitro: N/Ain vivo: Intravenous injection of 30 micrograms/kg of B-HT 920 into cats lead initially to an increase in blood pressure and then to a long-lasting decrease in blood pressure and heart rate. Vagally mediated reflex bradycardia elicited by angiotensin injection in beta-adrenoceptor-blocked dogs was facilitated by intracisternal injection of 10 micrograms/kg B-HT 920.
(-)-OSU6162 (PNU96391) hydrochloride is a dopamine stabilizer. (-)-OSU6162 hydrochloride acts as partial agonist at 5-HT2A and is a dopamine D2 antagonist. (-)-OSU6162 hydrochloride can be used for the research of aggression and irritability[1][2].
Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity[1].
PNU-96415E is a selective D4/5-HT2A antagonist. PNU-96415E may have potential antipsychotic efficacy[1].
Lumateperone (ITI-007) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia[1][2][3].
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.
Piribedil D8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
Brexpiprazole D8 (OPC-34712 D8) is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM)[1][2].
Bifeprunox mesylate 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 mesylate is an antipsychotic for the research of schizophrenia[1][2].
Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia[1].
JHW007 hydrochloride is the hydrochloride of JHW007. JHW007 is an antagonist of cocaine[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].
Desmethyl cariprazine is an active metabolite of Cariprazine[1]. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM)[2].
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].