human d4 receptor

L-741626 (3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole) 是D2多巴胺受体选择性拮抗剂，对人 D2、D3 和 D4 受体的Ki 分别为 2.4、100 和 220 nM。

L-745870 hydrochloride 是可透过血脑屏障的、选择性的、具有口服活性的多巴胺 D4受体拮抗剂，Ki=0.43 nM。它对 D2(Ki 为 960 nM) 和 D3(Ki 为 2300 nM) 受体的亲和力相对较弱，对 5-HT2受体，sigma 位点和 α-肾上腺素受体表现出中等亲和力。

Iloperidone (HP 873) 是一种D2 5-HT2受体拮抗剂，是非典型抗精神病药，可治疗精神分裂症。

ABT 724 trihydrochloride 是一种有效的选择性 D4 受体激动剂（EC50 = 12.4 nM，14.3 nM 和 23.2 nM，分别对人、大鼠和雪貂）。 ABT-724 trihydrochloride 可用于勃起功能障碍研究。

Sonepiprazole 是D4多巴胺受体选择性拮抗剂，与rD4多巴胺受体，hD4.2多巴胺受体，rD2多巴胺受体和组胺H1受体结合的Ki 分别为 3.6、10.1、5147 和 7430 nM。

GR 103691 是选择性的多巴胺 D3受体拮抗剂，Ki=0.4 nM。它对人多巴胺 D3的选择性超过 D4和 D1的 100 倍以上。

L-745870 是一种可透过血脑屏障且具有口服活性、选择性和高效性的多巴胺 D4 受体拮抗剂，抑制 D2 受体、5-HT2 受体和 α-肾上腺素受体，可用于研究神经系统疾病。

ABT-670 is a selective agonist of dopamine D4 receptor. For human D4, ferret D4, and rat D4, the EC50 values are 89 nM, 160 nM, and 93 nM , respectively.

Loxapine succinate (Loxapac) 是D2 D4多巴胺受体，5-羟色胺受体抑制剂，用于精神分裂症。

Fananserin 是一种有效的、特异性的、口服活性的 5-HT2 拮抗剂（大鼠 5-HT2A 的 Ki = 0.37 nM）。 Fananserin 是人 D4 受体的拮抗剂 (Ki = 2.93 nM)。

Verlukast is an (R)-enantiomer of MK-571 and a potent and selective LTD4 receptor antagonist. Verlukast showed [3H]leukotriene D4 binding in guinea-pig (IC50 = 3.1 +/- 0.5 nM) and human (IC50 = 8.0 +/- 3.0 nM) lung homogenates and dimethyl sulfoxide diffe

Loxapine 是 D2DR 和 D4DR 抑制剂和5-羟色胺能受体拮抗剂，是一种抗精神病药物，主要用于治疗精神分裂症。

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

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).

SRA880 is a non-peptide somatostatin sst(1) receptor antagonist which displays a significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d)= 6.0) or a wide range of neurotransmitter receptors, except for the human dopamine

SRA880 is a non-peptide antagonist of somatostatin sst1-receptor. SRA880 displayed significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d) < or = 6.0). SRA880 shows a certain binding affinity to the human dopamine D4 re

SV-156 is a highly selective antagonist of dopamine receptor 2 (D2).

U-101958 Maleate is a ligand of dopamine D4 receptor. U-101958 Maleate also binds to a large sigma1 receptor-like component in SK-N-MC neuroblastoma cells and human cerebellum with high affinity.

A-381393 是选择性、可透过血脑屏障的多巴胺 D4受体拮抗剂，对人多巴胺 D4.4，D4.2和 D4.7受体的 Ki 分别为 1.5，1.9 和 1.6 nM，选择性是对 D1，D2，D3，D5多巴胺受体的 2700 多倍，对 5-HT2A 的选择性适中，Ki=370 nM。

Ropinirole (SKF 101468) 是一种具有口服活性和高效性的 D3 D2 受体激动剂，具有抗肌萎缩侧索硬化症作用。Ropinirole 可用于研究帕金森氏病。

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

N-Despropyl ropinirole is an active metabolite of the dopamine D2 receptor agonist ropinirole. It increases extracellular acidification rates in CHO cells expressing human dopamine D2, D3, and D4 receptors (EC50s = 0.63, 0.063, and 1.23 µM, respectively). N-Despropyl ropinirole is also a potential impurity found in commercial preparations of ropinirole.

6-hydroxy Buspirone是抗焦虑化合物buspirone的活性代谢产物，通过细胞色素P450（CYP）亚型CYP3A4从buspirone转化而来。该化合物在大鼠海马和背侧缝核的5-羟色胺（5-HT）受体亚型5-HT1A上具有亲和力（EC50s分别为4和1 µM），并作为多巴胺D2、D3、D4受体拮抗剂（IC50s分别为3.1、4.9、和0.85 µM）。同时，它还以浓度依赖性方式抑制表达人类转运体的S2近端小管细胞中的有机阳离子转运体1（OCT1）、OCT2和OCT3。

CELT-426是一种高效且部分选择性的荧光hD2多巴胺受体拮抗剂，其Kivalue分别针对D2、D3和D4多巴胺受体，在放射配体结合实验中分别为89.3 nM、194.8 nM和263.6 nM。CELT-426可作为荧光多巴胺受体探针，在荧光结合实验、活细胞成像、流式细胞术及荧光偏振实验中使用。它是GPCR放射性标记配体的理想替代品。激发和发射峰值（λ）分别为560 nm和571 nm。这些波长适合作为TR-FRET实验中的受体染料，与CoraFluor1 TR-FRET供体一起使用。