Alizapride HCl是一种多巴胺受体拮抗剂，用于治疗恶心和呕吐。 了解更多

Azaperone是一种具有镇静和止吐作用的吡啶基哌嗪和丁苯酮类抗精神病药，主要在兽药中用作镇定剂。 了解更多

Azasetron HCl是一种选择性的5-HT3受体拮抗剂，IC50为0.33 nM，用于治疗癌症化学疗法引起的恶心和呕吐。 了解更多

Azilsartan medoxomil是一种口服给药的1型血管紧张素II受体拮抗剂，IC50为0.62 nM。 了解更多

Cyclizine 2HCl是具有组胺H1受体拮抗剂活性的哌嗪衍生物。 了解更多

A-438079 HCl是一种竞争性P2X7受体拮抗剂（抑制人重组P2X7细胞系中Ca2+流入的pIC50 = 6.9）。在其他P2受体上没有活性（IC50 > 10 uM）。 了解更多

MK-6096 (Filorexant)是目前正处于失眠临床开发中的口服生物利用型有效且选择性可逆的OX（1）R和OX（2）R拮抗剂。MK-6096表现出对人OX（1）R和OX（2）R的有效结合和拮抗作用（结合时<3 nM，FLIPR中为11 nM），对超过170个受体和 酶。 了解更多

Vipadenant，也称为BIIB014，CEB-4520，是针对帕金森氏症的有效，选择性和口服腺苷A2A受体拮抗剂。Vipadenant在帕金森氏病的常用模型中显示出强大的口服活性。 了解更多

Theophylline-7-acetic acid是腺苷受体拮抗剂，是黄嘌呤类化学物质的兴奋剂。 了解更多

Alloxazine是A2受体拮抗剂，其对A2B受体的选择性比A2A受体高约10倍。 了解更多

Flopropione是5-HT1A受体拮抗剂，也是儿茶酚-邻甲基转移酶（COMT）抑制剂。 了解更多

Asapiprant，也称为S-555739，是一种有效的选择性DP1受体拮抗剂。Asapiprant对DP1受体表现出高亲和力和选择性。 了解更多

CGRP 8-37 (human)是人降钙素基因相关肽（hCGRP）片段，也是CGRP受体的拮抗剂。序列：Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn- Val-Gly-Ser-Lys-Ala-Phe；VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF。 了解更多

Solifenacin是一种新型毒蕈碱受体拮抗剂，M1，M2和M3受体的pKis分别为7.6、6.9和8.0。 了解更多

PMX-205是一种环状六肽，可作为C5a受体的强效拮抗剂（C5aR；IC50 = 31 nM）。 了解更多

Esaxerenone（CS-3150,XL-550）是一种非甾体类抗盐皮质激素，可作为盐皮质激素受体（MR）（醛固酮受体）的高度选择性沉默拮抗剂，对该受体的选择性是其他受体的1000倍以上类固醇激素受体，相对于现有的抗盐皮质激素螺内酯和依普利酮，与MR的亲和力分别高4倍和76倍。 了解更多

Tradipitant，也称为VLY-686和LY686017，是第二代神经激肽1受体拮抗剂，在临床前焦虑模型中表现出活性。 了解更多

MRS1177是一种有效的选择性人腺苷A3受体（hA3AR）拮抗剂，Ki为0.3 nM。 了解更多

MRS1186是一种有效的选择性人腺苷A3受体（hA3AR）拮抗剂，Ki为7.66 nM。 了解更多

(-)-Securinine是一种最初从S. suffructicosa分离的生物碱。Securinine是一种特定的GABA受体拮抗剂，已发现在体内具有显着的CNS活性。 了解更多

GSK-269984A是新型的EP1受体拮抗剂。pIC50 值为 7.9。 了解更多

7CKA是在甘氨酸位点起作用的NMDA受体拮抗剂。 了解更多

JNJ-39758979是组胺H4受体拮抗剂，Ki为12.5 nM。 了解更多

PHTPP是基于吡唑并[1,5-α]嘧啶的配体，其作为雌激素ERβ受体的完全拮抗剂，其选择性是ERα的36倍。 了解更多

Neu-2000是可能用于治疗中风的NMDA受体拮抗剂。 了解更多

Cgp 52432是GABA-A受体拮抗剂。 了解更多

RO-1138452是一种有效且选择性的IP（前列环素）受体拮抗剂，对IP受体具有高度亲和力。 了解更多

TCS-OX2-29 HCl是一种选择性OX2受体拮抗剂，IC50值为40 nM。 了解更多

Volananserin是高度选择性的5-HT2A受体拮抗剂。 了解更多

AF 12198是人I型白介素1（IL-1）受体的有效选择性拮抗剂。 了解更多

Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). 了解更多

Montelukast (trade name Singulair) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. 了解更多

AZD-4282, also known as aminoacetic acid and glycine, is a N-methyl-D-aspartate (NMDA) receptor antagonist potentially for the treatment of neuropathic pain. 了解更多

Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine. 了解更多

Icatibant (HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively. 了解更多

Pizotifen is a serotonin antagonist which acts mainly at the 5-HT1, 5-HT2A, and 5HT2C receptors with some antihistamine activity. 了解更多

Mequitazine is a potent histamine H1 antagonist or antihistamine. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. 了解更多

ML401 is an antagonist of the EBI2 receptor with an IC50 of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC50=6.24 nM). ML401 shows good stability and no toxicity. 了解更多

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. 了解更多

NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. 了解更多

BMS-193885 is a potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over ??1, α1, Y2, Y4 and Y5 receptors respectively. 了解更多

PF-04634817 is an orally administered CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema. 了解更多

AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC50 of 38 nM for hLPA5. AS2717638 also significantly improves PGE2-, PGF2α-, and AMPA-induced allodynia. 了解更多

ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM. 了解更多

AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM. 了解更多

GW 766994 is a specific and oral chemokine receptor-3 (CCR3) antagonist, which has entered clinical trial for asthma and eosinophilic bronchitis. 了解更多

AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist. 了解更多

PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells. 了解更多

UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM). 了解更多