human d1 receptor

PF2562 is a dopamine D1 ligand. It is used as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor (Ki: 113 nM). PF2562 shows activity against human D1 cAMP (EC50: 568 nM in HTRF assay).

LE 300 是选择性多巴胺 D1 样受体拮抗剂，作用于人多巴胺 D1 和 D5 受体的Kis 分别为 1.9 nM 和 7.5 nM。在大鼠尾动脉实验中，它作用于5-HT2A 受体的pA2 为 8.32。

NCGC00135472 (DRV1 (GPR32) agonist C2A)是具有促分解功能的人Resolvin D1受体激动剂,可在β阻滞素和 cAMP 测定中激活人溶解蛋白 D1 受体 DRV1 GPR32 受体，EC50 分别为 0.37 uM 和 0.05 uM。NCGC00135472在过表达重组DRV1的细胞中引起快速阻抗变化，刺激血清处理的酶聚糖的吞噬作用。

Chlorprothixene (Truxal) 是一种多巴胺和组胺受体拮抗剂，具有抗精神病作用。它高亲和力地结合人 D1，D2，D3，D5，H1 受体，Ki 分别为 18 nM，2.96 nM，4.56 nM，9 nM 和 3.75 nM。

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。

UCM-1306 是具有口服活性的人多巴胺 D1 受体变构调节剂 (PAM)。UCM-1306 增加结合在人和小鼠 D1 受体的内源性多巴胺 (DA) 效应。UCM-1306可以改善运动症状，解决与长期帕金森病(PD) 相关的关键共病认知障碍。

Chlorprothixene hydrochloride (Truxal hydrochloride) 是一种多巴胺和组胺受体拮抗剂，具有抗精神病作用，高亲和力地结合人 D1，D2，D3，D5，H1 受体，Ki 分别为 18 nM，2.96 nM，4.56 nM，9 nM 和 3.75 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。

LY3154207 is a subtype selective, potent, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).

PF-06256142 is a potent and selective orthosteric D1 receptor agonist(D1 EC50=30 nM ).

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

Iloperidone metabolite P95 is a metabolite of the atypical antipsychotic iloperidone . It binds to the serotonin (5-HT) receptor subtype 5-HT2A and α1-, α2B-, and α2C-adrenergic receptors with mean Ki values of 7.08, 21.38, 83.18, and 47.86 nM, respectively, but does not cross the blood-brain barrier.

Protectin D1 (also known as neuroprotectin D1 when produced in neuronal tissues) is a DHA-derived dihydroxy fatty acid that exhibits potent protective and anti-inflammatory activities. 10(S),17(S)-DiHDHA is a DHA metabolite, also referred to as protectin DX (PDX). It is produced by an apparent double lipoxygenase (LO)-mediated reaction in murine peritonitis exudates, in suspensions of human leukocytes, or by soybean 15-LO incubated with DHA. It differs from protectin D1 with respect to the stereochemistry of the C-10 hydroxyl and the double bond configuration at the 13 and 15 positions. 10(S),17(S)-DiHDHA blocks neutrophil infiltration in murine peritonitis by 20-25% at a dose of 1 ng mouse. It also inhibits platelet activation by both impairing thromboxane (TX) synthesis and TX receptor activation.

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。

DETQ是一种具有选择性、变构性和口服活性的多巴胺D1受体增强剂。在表达人类D1受体的HEK293细胞中，通过增加cAMP水平发挥作用，其EC50为5.8nM，Kb为26nM。DETQ对大鼠和小鼠的D1受体效力降低约30倍，对人类D5受体则无活性。