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。

Methylene Blue trihydrate (Basic blue 9) 是鸟苷酸环化酶，单胺氧化酶 A 和 NO 合酶抑制剂。它是血管加压药，在医疗中通常用作染料。它具有抗伤害感受，抗疟疾，抗抑郁和抗焦虑作用，可用于高铁血红蛋白血症，神经退行性疾病和异环磷酰胺引起的脑病的研究。

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。

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。

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。

Rosmanol 能够显著抑制脂多糖诱导的 INOS、COX-2 的表达，抑制低密度脂蛋白的氧化，并具有抗炎作用。

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 is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

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。

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。

JWH 030 is a potent naphthoyl pyrrole cannabimimetic, exhibiting higher affinity for the CB1 receptor (EC50= 30.5 nM in rats, Ki= 87 nM in mice) compared to CB2 (EC50= 552 nM in human CB2 receptors). The compound demonstrates significant in vivo potency in mouse models, specifically in spontaneous activity and tail flick assays (antinociception) with an ED50 value of 26.8 μM/kg. Furthermore, JWH 030 dose-dependently reduces electrically-induced contractions in the mouse vas deferens, with an IC50 of 3.38 nM, highlighting its effective modulatory effects. This compound is designated for forensic or research applications.