occlusion

Pramipexole (SND 919) 是能够透过血脑屏障的 D2 型多巴胺受体的选择性激动剂，对 D2 型受体、D2、D3、D4亚型受体的Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM。它可用于研究帕金森综合症和腿多动综合征。

Pramipexole dihydrochloride hydrate (Mirapex) 是选择性的，具有血脑屏障 (BBB) 渗透性的 D2 型多巴胺受体激动剂，对 D2 型受体、D2、D3、D4亚型受体的 Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM，可用于研究帕金森综合症和腿多动综合征。

PHA 568487 free base 是一种选择性的 α7 烟碱乙酰胆碱受体激动剂，可用于减缓神经炎症。

Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。

CaCCinh-A01 是钙激活氯离子通道和TMEM16A 抑制剂，IC50值分别为 10 和 2.1 μM。

TGX-115是一种细胞渗透性和有效的PI 3-K 异构体p110β p110δ抑制剂(对p110β IC50值为 0.13 μM, 对p110δ值为0.63 μM），是一种调节血小板粘附过程的酶，可抑制磷酸肌苷（PI）3-激酶，可用来治疗冠状动脉闭塞、中风、急性冠状动脉综合征、急性心肌梗塞、血管再狭窄、动脉硬化和不稳定心绞痛等心血管疾病 。

Lifarizine (RS-87476) 是一种钙钠通道拮抗剂， 在简化的大鼠双血管闭塞存活模型中显示出神经保护活性。

Piclozotan (anhydrous) 是一种 5-HT1A 受体激动剂，在短暂的大脑中动脉闭塞（t-MCAO）模型中表现出显着的神经保护活性,可以改善晚期帕金森病患者的运动并发症。

Pinokalant (LOE-908) 是一种新型非选性阳离子通道抑制剂。Pinokalant 在体内实验中可显著减少皮质梗死体积，可改善缺血半影区的代谢和电生理状态，可减少大鼠大脑中动脉闭塞后急性期磁共振图像上的病变大小。Pinokalant是一种潜在的SARS-CoV-2蛋白酶抑制剂，可用于研究脑卒中。

MTP 131 acetate 是一种小的线粒体靶向四肽。

Coumetarol (Dicumoxane) 是维生素 K 拮抗剂，也是一种口服抗凝剂，可用于研究动脉血栓阻塞。

SMND-309 is a metabolite of salvianolic acid B. It also shows neuroprotective effects in cultured neurons and in permanent middle cerebral artery occlusion rats.

Compound Y12 (Neuroprotective agent 6) 是一种具备抗氧化性的神经保护剂。在氧糖剥夺 复氧 (OGD R) 诱导的细胞模型及短暂性大脑中动脉闭塞 (tMCAO) 诱导的动物模型中，Compound Y12 展现出卓越的神经保护能力。此外，该化合物对Cu2+也具有明显的金属螯合作用。

ASP8731 作为一种选择性的BACH1抑制剂，能有效抑制炎症和血管闭塞，同时在镰状细胞病治疗中诱导胎儿血红蛋白的生成。

Fostedil is a calcium channel antagonist. KB-944 increased regional segment function in normal and ischemic regions and maintained distal coronary artery perfusion pressure, coronary flow and transmural regional myocardial blood flow during partial corona

LY 215490 is a selective, competitive and systemically active antagonist of AMPA receptor. LY 215490 has neuroprotective effect against focal ischaemia in a model of permanent MCA occlusion in the rat.

TCV-309 is an inhibitor of platelet activating factor (PAF). TCV-309 reduces graft PMN infiltration and enhances early function of 24-hour-preserved rat kidneys with long warm ischemia. TCV-309 attenuates the priming effects of bronchoalveolar macrophages

Porfimer sodium is t he sodium salt of a mixture of oligomers formed by ether and ester linkages of up to eight porphyrin units with photodynamic activity. Absorbed selectively by tumor cells, porfimer produces oxygen radicals after activation by 630 nm w

(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage of the area at risk in a canine model of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) occlusion when administered at a dose of 0.128 mg kg prior to occlusion or reperfusion.[5] Reference：[1]. Chacos, N., Falck, J.R., Wixtrom, C., et al. Novel epoxides formed during the liver cytochrome P-450 oxidation of arachidonic acid. Biochem. Biophys. Res. Commun. 104(3), 916-922 (1982).[2]. Oliw, E.H., Guengerich, F.P., and Oates, J.A. Oxygenation of arachidonic acid by hepatic monooxygenases. Isolation and metabolism of four epoxide intermediates. J. Biol. Chem. 257(7), 3771-3781 (1982).[3]. Jiang, J.-X., Zhang, S.-J., Xiong, Y.-K., et al. EETs attenuate ox-LDL-induced LTB4 production and activity by inhibiting p38 MAPK phosphorylation and 5-LO BLT1 receptor expression in rat pulmonary arterial endothelial cells. PLoS One 10(6), e0128278 (2015).[4]. Oltman, C.L., Weintraub, N.L., VanRollins, M., et al. Epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids are potent vasodilators in the canine coronary microcirculation. Circ. Res. 83(9), 932-939 (1998).[5]. Nithipatikom, K., Moore, J.M., Isbell, M.A., et al. Epoxyeicosatrienoic acids in cardioprotection: Ischemic versus reperfusion injury. Am. J. Physiol. Heart Circ. Physiol. 291(2), H537-H542 (2006).

Thrombin receptor peptide ligand is antagonist of the thrombin receptor (EC50s = 16-33 μM to inhibit platelet aggregation in vitro). It inhibits α-thrombin and platelet aggregation induced by thrombin receptor activating peptide in vitro when used at a concentration of 32 μM but does not affect platelet aggregation induced by ADP or collagen. It also inhibits thrombin- and TRAP-induced proliferation of vascular smooth muscle cells (VSMCs). Thrombin receptor peptide ligand (100 μmol/kg bolus, i.v., plus 900 μmol/kg infusion) inhibits arterial thrombosis in a rabbit model of partial carotid artery occlusion without increasing bleeding time.

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.1 1.Ikeda, H.O., Sasaoka, N., Koike, M., et al.Novel VCP modulators mitigate major pathologies of rd10, a mouse model of retinitis pigmentosaSci. Rep.45970(2014) 2.Kinoshita, H., Maki, T., Yasuda, K., et al.KUS121, a valosin-containing protein modulator, attenuates ischemic stroke via preventing ATP depletionSci. Rep.9(1)11519(2019)

Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid receptor antagonist naltriben but not the δ1-opioid receptor antagonist BNTX.3Intrathecal administration of deltorphin II (15 μg animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.4 1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998)

L-Palmitoylcarnitine chloride (Palmitoyl-L-carnitine chloride)是一种脂肪酸代谢产物，具有抗血栓形成的作用，通过抵消tMCAO模型中的脑内血栓形成来保护小鼠免受缺血性中风。L-Palmitoylcarnitine chloride抑制心脏中的Na K泵，抑制 FeCl 3诱导的动脉血栓形成，减轻了短暂性大脑中动脉闭塞（tMCAO）小鼠模型的脑内血栓形成和炎症。

N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.