antinociception

BIMU 8 是 5-HT4 的选择性激动剂，对野生型 5HT4 受体、T3.36A 和 W6.48A 突变体 5-HT4 的 EC50 分别为 18 nM、77 nM 和 540 nM。

Deoxylimonin (NSC 314317) 是一种分离自葡萄柚籽中的三萜化合物。它是一种母体衍生物，其抗癌、缓解疼痛和抗炎活性比母体化合物强。

Allopurinol (Zyloric) 是一种黄嘌呤氧化酶(XO)抑制剂，IC50=7.82±0.12 μM。

A-803467 是有效的、选择性的河豚毒素不敏感型Nav1.8 钠通道阻断剂 。它在炎症性疼痛和神经性疼痛模型中有缓解疼痛作用。它通过与 ATP-binding cassette subfamily G member 2 (ABCG2) 转运蛋白的相互作用，增强了传统抗癌物的化疗敏感性。

Allopurinol Sodium 是黄嘌呤氧化酶抑制剂，其IC50= 0.2~50 μM。它能够抗利什曼原虫，也可用于研究痛风以及高尿酸血症。

PMSF (Phenylmethylsulfonyl fluoride) 是一种丝氨酸/半胱氨酸蛋白酶不可逆抑制剂，常用于制备细胞裂解物。

Adenosine A1 receptor activator T62 是腺苷 A1 受体的变构增强剂，有镇痛作用。

β-Endorphin (1-27) (human) acetate 存在于大脑垂体和下丘脑中，具有镇痛活性。 β-Endorphin (1-27) (human) acetate 是一种阿片受体激动剂，对 μ-阿片受体和 δ-阿片受体具有较好的亲和力。

AR-C102222 hydrochloride is a competitive, orally active, and highly selective inducible nitric oxide synthase (iNOS) inhibitor (IC50: 37 nM). It has antinociception and anti-inflammatory activities.

JDTic Dihydrochloride是一种高亲和力和选择性的κ-opioid receptor(KOR)拮抗剂，能够阻断dynorphin-KOR信号，具有抗抑郁、抗焦虑及抑制可卡因与尼古丁复吸的作用。

A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM, and it has antidepressant and antinociception effects[1][2].

Paynantheine是一种在Mitragyna speciosa中发现的生物碱，具有抗伤害活性。Paynantheine也是一种5-HT1AR和5-HT2BR激动剂，可引起大鼠下唇收缩和具有抗刺激作用。

KOR agonist 5 (Compound 10a) 是一种KOR/MOR调节剂，对KOR具有激动活性，而对MOR则展示拮抗性质。它能够有效阻止吗啡引起的抗伤害感受作用以及抑制肠道运动。KOR agonist 5 可应用于物质使用障碍 (SUD) 的研究。

Tingenone is a pentacyclic triterpene. It induces peripheral antinociception due to opioidergic activation.

Leucylarginine hinders antinociception induced by L-arginine.

ONO-1714 is a inducible nitric oxide synthase (NOS-2) inhibitor. ONO-1714 reduces hyperoxic lung injury in mice. ONO-1714 attenuates inflammation-related large bowel carcinogenesis in male Apc(Min/+) mice. ONO-1714 also inhibits neuronal NOS and exerts an

ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 is brain penetrant, increased the potency of orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, c

MS 15203是一种选择性 GPR171 激动剂,可增加吗啡的抗伤害感受，可有效减轻慢性疼痛,可减少雄性小鼠的慢性神经性和炎症性疼痛。

(R)-AM1241 binds to cannabinoid (CB) receptors and has greater than 100-fold selectivity for the CB2 over the CB1 receptor (Kis = 15 and 5,000 nM, respectively, in a membrane assay using human receptors). (R)-AM1241 acts as an agonist at human CB2 receptors (EC50 = 118 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 315 and 341 nM, respectively). Similar to the racemate AM1241 , (R)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (R)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone .

(S)-AM1241 binds to cannabinoid (CB) receptors and is selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively, in a membrane assay using human receptors). (S)-1241 acts as an agonist at human, rat, and mouse CB2 receptors but shows greater activity at human CB2 (EC50 = 131 nM) than at rat and mouse CB2 receptors (EC50 = 785 and 2,000 nM, respectively). Similar to the racemate AM1241 , (S)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (S)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone .

β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.

Paederosidic acid methyl ester 是 ATP 敏感的 K+channel 通道激活剂，分离自 P. scandens。它通过激活脑中和脊髓水平中 ATP 敏感型 K+通道提高了痛觉阈值，表现出显著的中枢缓解疼痛活性。

Gelsemine (Gelsemin) 是一种从中草药 Gelsemium elegans 中获得的生物碱，具有抗伤害和促进睡眠活性，可有效缓解慢性疼痛。

SC13 是一种新型的 mitragynine 类似物，具有低效Muopioid receptor 激动作用，具有麻醉作用和较轻的不良反应。