β antagonists

Celiprolol hydrochloride (Selectrol) 是一种选择性肾上腺素受体调节剂，是一种选择性的和具有口服活性的β1肾上腺素受体拮抗剂，具有部分β2激动剂活性，具有降压和抗心绞痛的作用。

Calcium-Sensing Receptor Antagonists I functions as an antagonist to the parathyroid hormone receptors that sense calcium.

Glucagon receptor antagonist -1 is a highly effective glucagon receptor antagonist.

Glucagon receptor antagonist -3 is a highly effective glucagon receptor antagonist.

Glucagon receptor antagonists-5 is an orally bioavailable indazole-based glucagon receptor antagonist (Ki: 32 nM). It has potential for the treatment of type 2 diabetes mellitus (T2DM).

Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist. It has a binding affinity of 18 nM and as a novel anticancer agent.

Glucagon receptor antagonist -2 is a highly effective glucagon receptor antagonist.

PF-06291874 (Glucagon receptor antagonists-4) 是口服有活性的胰高血糖素受体非肽类拮抗剂。它正用于研究 2 型糖尿病。

TSHR antagonist S37 是促甲状腺激素受体 (TSHR) 的选择性和竞争性拮抗剂。

TSHR antagonist S37a is a selective antagonist of thyrotropin receptor (TSHR), with potential for the treatment of Graves' orbitopathy.

TSHR antagonist S37b, the less potent enantiomer of TSHR antagonist S37a, exhibits minimal efficacy in inhibiting the thyrotropin receptor (TSHR). It is utilized in thyroid function research[1].

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .

SAE-14 是一种特异性的 GPR183 拮抗剂。在钙流动实验中，SAE-14 以 28.5 nM 的 IC50 抑制 GPR183 活性[1]。

CXCR4 antagonist and ACKR3 (CXCR7) agonist (EC50 = 350 nM for CXCR7).

WEHL-04 是一种中间体，用于制备（异喹啉基磺酰基）苯甲酸，作为 5 型 71-β-羟基类固醇脱氢酶 AKR1C3 的抑制剂。它还用于合成 2-氨基八氢环戊二烯-3a-羧酰胺作为有效的 CCR2 拮抗剂。

CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM 1 nM in β-arrestin assay CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1]. CXCR2-IN-2 (compound 68) (1-10 mg kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models[1]. [1]. Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61(6):2518-2532.

Pindolol-d7 是 Pindolol 的氘代化合物。Pindolol 的 CAS 号为 13523-86-9。Pindolol 是一种非选择性β-阻断剂，局部的β-肾上腺素能受体激动剂活性，也作为5-HT1A受体部分拮抗剂，Ki为33nM。它是非心脏选择性的，具有内在的拟交感神经作用。

23-O-β-D-Glucopyranosyl-20-isoveratramine，一种从荨麻提取的潜在抗过敏剂，含多种抑制剂，如COX-1、COX-2、5-脂氧合酶以及类胰蛋白酶抑制剂和H1 拮抗剂。这些成分对季节性过敏、过敏性鼻炎和其他炎症性疾病具有显著的抑制和预防作用。