human d2 receptor

L-745870 hydrochloride has excellent brain penetration. 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 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM. 

L-741626 (3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole) is a selective antagonist of D2 dopamine receptor (Ki: 2.4, 100, and 220 nM for human D2, D3 and D4 receptors respectively).

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Chlorprothixene (Truxal) is a typical antipsychotic drug of the thioxanthene class, which was the first of the series to be synthesized.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

Ropinirole hydrochloride (SKF-101468A) is a selective dopamine D2 receptors agonist (Ki: 29 nM). Ropinirole hydrochloride (SKF-101468A) is the hydrochloride salt form of ropinirole, a non-ergot dopamine agonist with antiparkinsonian property.

Sonepiprazole (PNU-101387G) is a chemical compound known for its selective antagonistic properties toward D4 dopamine receptors, exhibiting dissociation constants (Kis) of 3.6 nM and 10.1 nM for rat D4 (rD4) and human D4.2 (hD4.2) dopamine receptors, respectively; it shows significantly less affinity for rat D2 (rD2) dopamine and Histamine-H1 receptors, with Kis of 5147 nM and 7430 nM, respectively.

(+)-PD 128907 hydrochloride is an agonist of the D3 dopamine receptor.

Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Chlorprothixene hydrochloride (Truxal hydrochloride) brings strong blocking effects by blocking the 5-HT2 D1, D2, D3, histamine H1, muscarinic and alpha1 adrenergic receptors. Chlorprothixene hydrochloride s a typical antipsychotic drug of the thioxanthene (tricyclic) class.

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

L-745870 is an orally active, selective, and efficient dopamine D4 receptor antagonist that crosses the blood-brain barrier. It also inhibits D2 receptors, 5-HT2 receptors, and α-adrenergic receptors, useful in neurological disease studies.

Loxapine succinate (Loxapac), a D2DR and D4DR inhibitor, is utilized in schizophrenia.

RG-15 is an orally active dopamine receptor antagonist with high affinity for the human D2 receptor (pKi of 8.23) and human D3 receptor (pKi of 10.49). It inhibits dopamine-stimulated [35S]GTPγS binding with IC50 values of 21.2 nM in rat striatal membranes, 36.7 nM in mouse A9 cells expressing human D2L receptors, and 7.2 nM in CHO cells expressing human D3 receptors. RG-15 enhances dopamine turnover and synthesis in the striatum and olfactory bulb of mice, exhibiting antipsychotic activity.

Boc-MIF-1-Am (compound 2) acts as a human dopamine D2 receptor enhancer with an EC50 value of 17.82 nM and is a bioconjugate of melanostatin (MIF-1) and amantadine. At a concentration of 200 μM, Boc-MIF-1-Am exhibits slight neurotoxicity in SH-SY5Y cells.

Loxapine is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent,used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines).

(+)-AJ-76 is an antagonist of the dopamine autoreceptor, with a weak antagonistic effect on postsynaptic dopamine receptors. (+)-AJ 76 HCl can increase the synthesis and turnover of dopamine in the rat brain, and can also antagonize the sedative effect of low-dose apomorphine.

BGC20-761 is a selective 5-HT6 and dopamine receptor antagonist (human receptor K i values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM)), and a tryptamine analog with a high affinity for 5-HT(6) receptors, that can enhance long-term memory, with potential utility as an antipsychotic agent [1].

Iloperidone hydrochloride is a D(2)/5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

FAUC 213 is a selective full antagonist of the dopamine D4 receptor.

L 741742 is an effective and highly selective antagonist of the D4 dopamine receptor (Ki: 1700, 770, and 3.5 nM at cloned human D2, D3, and D4 receptors).