spinal cord injury

SRS16-86 是一种铁死亡抑制剂，可研究肾缺血再灌注损伤和脊髓损伤。它在体内比 Ferrostatin-1 对代谢和血浆更稳定。

Chroman 1 是高效的的ROCK 选择性抑制剂，对 ROCK2 (IC50=1 pM) 的抑制作用强于 ROCK1 (IC50=52 pM) 。它对MRCK 也有抑制作用，IC50为 150 nM。

Gacyclidine (OTO311) 是一种小分子 N-甲基-D-天冬氨酸(NMDA)受体拮抗剂。在耳蜗局部注射加西环定可抑制水杨酸盐引起的耳鸣，可用于治疗脑损伤、脊髓损伤和耳鸣。

Silperisone HCl (RGH-5002) 阻断细胞中的钠和钙通道，使肌肉细胞的兴奋度和收缩度降低，降低外周张力，充当肌肉松弛剂和外周血管扩张剂。 Silperisone HCl 可用于治疗脊髓损伤引起的复发性疼痛性肌阵挛、脑血管病引起的异常高肌张力、肌张力症状、锥体紧张综合征、多发性硬化症肌痉挛和脊髓炎。Silperisone 是钠通道蛋白2型α通道阻滞剂。Silperisone 是一种类似于tolperisone 的有机硅化合物，具有中枢作用的肌肉松弛剂特性。

Tirilazad mesylate (U 74006F) 是一种非糖皮质激素，是一种脂质过氧化抑制剂，具有抗病毒活性和神经保护活性。Tirilazad mesylate 能使细胞膜内病灶局限化，可减轻创伤、中风、缺血再灌注损伤引起的脊髓损伤，抑制狗体内毒素的作用，降低了内毒素诱导的肠系膜和肾脏 DO2 比容升高。Tirilazad mesylate 可用于研究神经系统疾病。

KCL-286是一种可口服且具有有效性的视黄酸受体β激动剂，可用于改善脊髓损伤(SCI)。

Peptide5 acetate 可减少脊髓损伤后的动物肿胀、星形胶质细胞增生和神经元细胞死亡。 Peptide5 acetate 显着降低啮齿动物离体模型中的脊髓损伤 (SCI) 程度。

ALLM (Calpain inhibitor II), a potent calpain and cathepsin protease inhibitor, not only prevents neuronal cell death but also enhances chronic neurological function following spinal cord injury (SCI)[1][2].

ALLM acetate（110115-07-6 Free base) 是一种有效的钙蛋白酶和组织蛋白酶抑制剂，不仅可以防止神经元细胞死亡，还可以增强脊髓损伤（SCI）后的慢性神经功能。

LY-266097作为一种选择性5-HT2BR拮抗剂，有效降低了触觉过敏，显示了其在缓解神经损伤引起的疼痛中潜在的治疗效果。此外，LY-266097还可以减轻神经损伤后背根神经节和脊髓中5-HT2B受体的上调。研究表明，LY-266097在神经病性疼痛途径的发展中具有潜在作用。

Leplinine (AIT-082, SPI-205) is a neurotrophic agent that may be used to treat Alzheimer's disease and spinal cord injury.

(±)12(13)-DiHOME is the diol form of (±)12(13)-EpOME , a cytochrome P450-derived epoxide of linoleic acid also known as isoleukotoxin. [1] It is formed from 12(13)-EpOME by soluble epoxide hydrolase (sEH) in neutrophils. [2] 12(13)-DiHOME is toxic to Sf21 cells expressing sEH and to lacZ-expressing control cells, unlike isoleukotoxin, which is only toxic to cells containing sEH.[1] [2] Levels of 12(13)-DiHOME are increased in rat spinal cord following burn injury, and it enhances cold tolerance, increases fatty acid uptake into brown adipocytes, and decreases serum triglyceride levels in mice. Levels are also elevated in bronchoalveolar lavage fluid (BALF) in humans following exposure to biodiesel exhaust and in exhaled breath condensate in patients with allergic asthma following allergen exposure.[5] [6] Plasma levels of 12(13)-DiHOME are increased immediately following moderate-intensity exercise in mice and humans, an effect that can be prevented by brown adipose tissue removal in the mouse.[7]

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)

Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 |Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats. Exp.Brain.Res. 235 3033 PMID:28725925 |Kim et al (2017) Characterising the mode of action of extracellular Connexin43 channel mimetic peptides in an in vitro ischemia injury model. Biochem.Biophys.Acta. 1861 68 PMID:27816754 |Tonkin et al (2017) Attenuation of mechanical pain hypersensitivity by treatment with Peptide5, a connexin-43 mimetic peptide, involves inhibition of NLRP3 inflammasome in nerve-injured mice. Exp.Neurol. 300 1 PMID:29055716

Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1 that can autoinduce production of antibacterial substances active against S. aureus when co-cultured at a low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro when used at concentrations of 16 and 32 μM. It increases phosphorylation of the PI3K substrate Akt, and neurite outgrowth induced by cyclo(L-Phe-L-Val) can be blocked by the PI3K inhibitor LY294002 . Cyclo(L-Phe-L-Val) enhances axon sprouting of calcitonin gene-related protein positive (CGRP+) primary afferents in the spinal cord following crush injury and of serotonin neurons in uninjured spinal cord. Cyclo(L-Phe-L-Val) is also a bitter taste component of cocoa and roasted coffee.

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs with ED50 values of 38 and 81 nmol kg, respectively. In a rat model of spinal cord injury, methoctramine suppresses bladder overactivity induced by the non-selective muscarinic acetylcholine receptor agonist oxotremorine M.[3]

Z-LEHD-FMK TFA is a specific and irreversible inhibitor of caspase-9, offering protection against detrimental reperfusion injury and moderating apoptosis. Additionally, Z-LEHD-FMK TFA demonstrates its neuroprotective potential in a rat model of spinal cord trauma.

NS309 是选择性钙依赖性钾离子通道 SK IK 的激活剂，在 BK 通道上没有激活作用。

Tirilazad是一种21-氨基类固醇非糖皮质激素，具有抑制脂质过氧化的能力。它对于脑或脊髓中因创伤、中风、缺血再灌注损伤所致的损害有减轻作用。此外，Tirilazad还展现出针对新型肺炎病毒的抗病毒活性，并在缺血性中风中提供神经保护，适用于蛛网膜下腔出血研究场景。

Hyp9为特异性激动剂，针对瞬时受体电位阳离子通道6（TRPC6），应用于脊髓损伤（SCI）的研究。

Peptide5 TFA，一种connexin 43模拟肽，能够降低动物脊髓损伤后的肿胀、抑制星形胶质细胞增生和神经元死亡。该化合物还可抑制NLRP3炎症小体，具有抗炎作用。

PTPσ Inhibitor, ISP 结合并抑制重组人PTPσ的信号传导，具有穿透细胞膜的能力，有助于缓解CSPG介导的脊髓损伤模型中轴突的生长抑制。该抑制剂能增强LPC引起的脊髓脱髓鞘损伤的髓鞘再生，并在MS动物模型中促进OPC的迁移、分化、髓鞘形成及功能恢复。

Unasnemab (MT-3921)，一种人源化IgG1单克隆抗体，与排斥引导分子A (RGMa) 结合，用以改善运动功能及促进神经再生，适用于脊髓损伤研究。

Phenylbenzothiazole-PEG4-OH (化合物1) 具有治疗脊髓损伤和促进脊柱形成的作用。