PAFR

48740 RP (RP 55779) 是血小板活化因子的拮抗剂。

Niranthin 是一种木脂素，具有广泛的药理活性。它是L. donovaniIB 拓扑异构酶的非竞争性抑制剂，可用于研究耐药利什曼病的治疗。

Tulopafant（RP 59227） 是一种有效的血小板活化因子 (PAF) 拮抗剂，可增加毛细血管通畅性并延长异体心脏移植的生存期。

CV-6209 是一种具有选择性和高效性的血小板活化因子 (PAF) 拮抗剂，具有抗增殖作用，部分抑制乙酰胆碱诱导的低血压，抑制 Paf 诱导的 PMN 或血小板聚集。CV-6209 具有抗幽门螺杆菌作用，可以抑制 PAF 引起的大鼠低血压。

(Rac)-Modipafant是一种可口服且具有选择性的血小板活化因子受体 (PAFR)拮抗剂，抑制 PAF 诱导的兔洗涤血小板聚集，可用于研究关节炎和大鼠肠系膜上动脉（SMA）缺血再灌注（I R）。

Yangambin 是从诸如番荔枝科植物中分离出来的呋喃木脂素，是选择性PAF 受体拮抗剂，通过调控Ca2+通道抑制 Ca2+流入，导致 [Ca2+]i 在血管平滑肌细胞和随后的外周血管舒张中减少，具有降压作用。

Ginkgolide B (BN-52021) 是一种萜类物质，是银杏叶中的重要的活性物质之一。

Zingiberen newsaponin 是分离自盾叶薯 (Dioscorea zingiberensis) 中。 它能够诱导血小板聚集。

Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) 从暹罗草中提取，通过 NF-κB 途径表现出抗炎活性。

Ferulamide (4-Hydroxy-3-methoxycinnamide) 是从巴豆中分离的阿魏酸衍生物，具有抗胆碱酯酶活性。

(-)-Denudatin B (Denudatin B) 源自 Magnolia fargesii。 (-)-Denudatin B 通过抑制胶原蛋白和凝血酶诱导的磷酸肌醇分解，在高浓度下具有非特异性抗血小板作用。

Apafant (WEB 2086) 是一种高效的血小板活化因子 (PAF) 拮抗剂，可阻断嗜酸性粒细胞活化，可用于研究豚鼠实验性过敏性结膜炎。

Rupatadine Fumarate (Rinialer) 是一种可口服的长效PAF H1受体的双抑制剂，Ki 值分别为 0.55 μM 和 0.1 μM。它可研究过敏性鼻炎和荨麻疹。

PAF C-18（十八烷 PAF）是一种天然存在的磷脂类分子，属于血小板活化因子（PAF）家族,作为细胞间信号传导分子，涉及血小板聚集、血管扩张和炎症反应。PAF C-18通过与其特异性G蛋白偶联受体（PAFR）结合参与止血和血栓形成过程，是内源性激动剂。

PAF-AN-1是一种新型有效的血小板激活因子受体 (PAF) 拮抗剂，参与研究过敏性死亡。

β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)

6-Deoxyjacareubin 具有有效的抗氧化和抗真菌活性。 6-Deoxyjacareubin 抑制血小板活化因子 (PAF) 受体，IC50 为 29.0 microM，可用于天然 PAF 受体拮抗剂的研究。

Kadsurin A 具有抗血小板活化因子活性。

Kadsulignan L shows in vitro antiviral effects on hepatitis B virus. It also shows moderate platelet-activating factor (PAF) antagonistic activities with the IC50 value of 2.6 x 10(-5) M.

Futoquinol is an anti-platelet activating factor principle from the stem part of Piper futokadsura (Piperaceae), the Chinese drug haifengteng.

6-Acetyl-2,2-dimethylchroman-4-one and vanillin exhibit anti-platelet aggregation activity induced by arachidonic acid in vitro.

Piperlotine C shows potent antiplatelet aggregation activity.

Hancinone C shows inhibitory activity against the platelet aggregation caused by PAF.

2-Hydroxy-3-methoxybenzoic acid glucose ester shows a potent antagonistic activity against platelet activating factor (PAF), it can prevent the mice from the PAF-induced death at a dose of 300 micrograms mouse.

Piperolactam C possesses anti-platelet aggregation activity in vitro. It can inhibit the growth of the fungi Cladosporium sphaerospermum and C. cladosporioides.

Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.

Cryptomeridiol is a potential skin-whitening agent, exhibits melanogenesis inhibitory activity on α-MSH-stimulated B16 melanoma cells. Cryptomeridiol has low activity against A. niger, T. mentagrophytes, and C. albicans. (-)-Cryptomeridiol also exhibits a significant and concentration-dependent inhibitory effect on PAF receptor binding, with inhibitory concentration (IC)(50) values of 17.5 uM.

Aristolactam AII has cytotoxic activity, it also shows platelet aggregation inhibitory activity.

1-Methoxyphaseollidin exhibits anti-Helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains. 1-Methoxyphaseollidin may show moderate cytotoxic activity against KB and L1210 cells. 1-Methoxyphaseollidin also shows inhibition of lysoPAF acetyltransferase activity.

Futoenone and a series of its derivatives have shown inhibitory activities against matrix metalloproteinases, the molecular modelings of these compounds indicate the preferred binding of the P2' site of the enzymes. Neolignan derivative compounds of the 2,4-diaryl-1,3-dithiolane and futoenone variety exhibit both platelet activating factor receptor(PAF)and 5-lipoxygenase antagonist activity.

(+)-Acuminatin exerts hepatoprotective activities, perhaps by serving as a potent antioxidant. (+)-trans-Acuminatin, and (+)-cis-acuminatin show weak activity against platelet aggregation with IC50 values of 108.5 and 90.02 uM, respectively. (+)-Acuminatin, and machilin G show dose-dependent potent inhibitory activities against PLCgamma1 in vitro with IC50 values ranging from 8.8 to 26.0 microM, the inhibition of PLCgamma1 may be an important mechanism for an antiproliferative effect on the human cancer cells, therefore, these inhibitors may be utilized as cancer chemotherapeutic and chemopreventive agents.

Pregomisin shows platelet-activating factor (PAF) antagonistic activity and the IC 50 value is 4.8x10(-5) M.

Cyclocommunol exhibits cytotoxicity against hepatocellular carcinoma (SMMC-7721) and gastric carcinoma (BGC-823 and SGC-7901) cell lines. It also shows strong inhibition of arachidonic acid (AA)- and collagen-induced platelet aggregation.

Spiradine F can significantly inhibit platelet-activating factor(PAF)-induced platelet aggregation in a concentration-dependent manner.

Bisdethiobis(methylthio)gliotoxin is a platelet activating factor (PAF) antagonist.

Epiyangambin is a phytotoxic lignan, it shows inhibition of seed germination of Agrostis stolonifera cv. penncross (Poaceae) and inhibition of development of Lactuca sativa L. (Asteraceae) seedlings in a microassay using 24-well plates. Epiyangambin exhibits significant inhibition of the transformation of murine epidermal JB6 cells, with the IC50 value of 0.15 microg mL. (+)-Epiyangambin also has anti-platelet aggregation activity.

Pinusolidic acid shows a potent inhibitory effect on platelet activating factor (PAF) binding to rabbit platelets (IC50 = 2.3 x 10(-5) M, 7.48 + - 2.11 micrograms ml).

Myrianthic acid shows anticancer activity, it shows inhibitory activities on foam cell formation in human monocyte-derived macrophages induced by acetylated low-density lipoproteins at a 50 uM concentration. Myrianthic acid is equivalently inhibitive as acetylsalicylic acid (IC50: 57.0 microM) on epinephrine induced platelet aggregation.

Piperenone is an insect antifeeding substance. It has anti-platelet-activating factor(PAF) activities, is a PAF-acether antagonist.

Piperlotine D shows potent antiplatelet aggregation activity.

Aristolactam BIII possesses anti-platelet aggregation activity in vitro, it also shows significant cytotoxic activity (IC50 values < 4 microg mL) against P-388, HT-29 and A549 cell lines in vitro.