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31

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9833	Opiranserin hydrochloride	P2X Receptor; GlyT; 5-HT Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Opiranserin hydrochloride 是甘氨酸转运蛋白 2 型 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂，IC50 分别为 0.86 和 1.3 μM。它显示对 rP2X3 的拮抗活性 (IC50=0.87 μM)。它正在开发为用于治疗术后疼痛的注射剂。
T6504	Flupirtine maleate Katadolon maleate,氟吡啶马来酸,马来酸氟吡汀	Potassium Channel; NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	Flupirtine maleate (Katadolon maleate) 是可透过血脑屏障的、具有口服活性的非阿片类化合物。它是间接 NMDAR 拮抗剂，可用于缓解疼痛的研究，具有神经保护特性。
TP1559L	Ziconotide Acetate (107452-89-1 free base) 醋酸齐考诺肽,Prialt,Ziconotide Acetate	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Ziconotide Acetate (107452-89-1 free base) (Prialt) 是一种镇痛剂，已用于治疗神经性和非神经性疼痛。 Ziconotide 通过与位于伤害感受通路初级传入神经元末端部分的 N 型钙通道结合起作用，因此通过有效的镇痛作用减少突触传递。
T16399	Opiranserin	P2X Receptor; GlyT; 5-HT Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Opiranserin 是一种非阿片类和非 NSAID 镇痛候选药物，是 2 型甘氨酸转运蛋白 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂，IC50分别为 0.86 和 1.3 μM。它可用于术后疼痛的研究，对 rP2X3 有拮抗作用，IC50为0.87 μM。
T3720	Tebanicline hydrochloride 替巴克兰盐酸盐,ABT-594 hydrochloride,Ebanicline hydrochloride	AChR	Neuroscience
	Tebanicline hydrochloride (Ebanicline hydrochloride) 是一种有效的合成烟碱（non-opioid）镇痛药。
T39349	Vocacapsaicin hydrochloride CA-008 hydrochloride	TRP/TRPV Channel	Membrane transporter/Ion channel
	Vocacapsaicin hydrochloride (CA-008 hydrochloride) 是非阿片类 TRPV1 激动剂，是辣椒素的原料，可用于缓解疼痛。
T0470	Nefopam hydrochloride 盐酸奈福泮,Fenazoxine hydrochloride,Nefopam HCl	Wnt/beta-catenin; Sodium Channel	Cytoskeletal Signaling; Membrane transporter/Ion channel; Stem Cells
	Nefopam hydrochloride (Nefopam HCl) 作用于体外和体内间充质细胞β-连环蛋白水平，是一种中枢性但非阿片类缓解中度和重度疼痛。
T39529	AT-121 hydrochloride	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AT-121 hydrochloride 是一种 nociception 和 mu 阿片受体 (mu opioid receptor)的双重激动剂，Ki 值分别为 3.67 和 16.49 nM。AT-121 hydrochloride 是一种安全、无成瘾性且科缓解疼痛的化合物，具有抗伤害和止痛活性。
T8414	SNC 80 Snc-80,SNC80,NIH 10815	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	SNC 80 (NIH 10815) 是有效的，高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂，Ki 为1.78 nM，IC50 为 2.73 nM。SNC80 还以 EC50 为 52.8 nM 来选择性激活 HEK293 细胞中的 μ-δ 异聚体。SNC80 具有抗伤害性，抗痛觉过敏和抗抑郁样作用，并可用于多种头痛症的研究。
T37610	AT-121	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AT-121 是一种双重μ-阿片和神经肽受体部分激动剂（Kis 分别为 16.49 和 3.67 nM）。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合（EC50s 分别为 19.6 和 34.7 nM）。AT-121（0.003-0.03 mg/kg）能以剂量依赖的方式降低辣椒素诱导的热异感，但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中，AT-121 每次注射剂量为 0.3 至 10 μg/kg，它缺乏强化作用（一种潜在的滥用标志），不能减少食物颗粒的强化作用。AT-121（0.01 或 0.03 毫克/千克）不会诱发恒河猴的超痛觉，超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药，具有抗伤害和止痛作用。
T27253	Elismetrep
	Elismetrep is a non-opioid analgesic.
T23972	DDD028 DDD 028,DDD-028
	DDD-028 is a potential non-opioid and non-cannabinoid analgesic. It was used for treating neuropathic and inflammatory pain.
T34784	TAN67 SB-205607 dihydrobromide,SB 205607 dihydrobromide,SB205607 dihydrobromide,TAN-67,TAN 67
	TAN67 is the first effective selective non-peptide delta1 opioid receptor.
T25690	Levallorphan tartrate Lorfan
	Levallorphan tartrate is an opioid antagonist with properties similar to those of NALOXONE. Levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid ce
T31631	Enkephalin-leu, ala(2)-ser(6)- DALES,2-Ala-6-ser-leu-enkephalin
	Enkephalin-leu, ala(2)-ser(6)- is an active compound at the delta (non-complexed) opioid receptor.
T26475	A-286501
	A-286501 is an orally active adenosine kinase inhibitor (IC50=0.47 nM). A-286501 effectively attenuates nociception by a non-opioid, non-non-steroidal anti-inflammatory drug ADO, receptor mediated mechanism.
T23313	SB 205607 dihydrobromide	Others	Others
	non-peptide δ1 opioid receptor agonist
T70503	Exp 631
	Exp 631 is a centrally-acting non-opioid analgesic; exhibits serotonin and norepinephrine reuptake inhibiting activities.
T39747	Nepinalone hydrochloride
	Nepinalone hydrochloride, a non-opioid antitussive, is an alchilaminate derivative of β-tetralone. This orally active compound effectively suppresses coughing.
T39348	Vocacapsaicin CA-008,Vocacapsaicin
	Vocacapsaicin (CA-008), a prodrug of Capsaicin and a first-in-class non-opioid TRPV1 agonist, offers significant and enduring pain relief.
T2806L	Lappaconitine HCl Lappaconitine hydrochloride
	Lappaconitine HCl is a centrally acting non-opioid analgesic and class-I antiarrhythmic. It acts by binding to the site-2 receptor and irreversibly blocking hH1 sodium channels.
T69422	Flupirtine HCl
	Flupirtine HCl is the salt form of Flupirtine, also known as W-2964, an aminopyridine that functions as a centrally acting non-opioid analgesic. It first became available in Europe in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor. Like nefopam, it is unique among analgesics in that it is a non-opioid, non-NSAID, non-steroidal centrally acting analgesic. Flupirtine is a selective neuronal potassium channel opener that also has NMDA re...
T68933	Gaboxadol hydrobromide
	Gaboxadol hydrobromide is a GABA agonist. It is an inhibitor of GABA uptake systems. Gaboxadol can also be a non-opioid analgesic and a novel type of hypnotic.
T12169	Naltrindole hydrochloride	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Naltrindole hydrochloride 是一种选择性的非肽类 δ 阿片受体拮抗剂 (Ki = 0.02 nM)。
T27363	FR 64822 FR-64822,FR64822
	FR64822(N-(4-pyridylcarbamoyl)amino 1,2,3,6,-tetrahydropyridine), a novel non-opioid antinociceptive compound, displays antinociceptive activities in a variety of assays with mice and rats. It has a strong antinociceptive activity in the acetic acid writh
T71772	Bicifadine free base
	Bicifadine, also known as DOV-220075, CL 220,075, is a SNDR inhibitor potentially for the treatment of lower back pain. Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs. While the drug is purported to be a serotonin (SERT) and noradrenaline transporter (NET) inhibitor, it also has effects at the dopamine transporter (DAT), effectively making it a broad...
T38192	Unifiram	Others	Others
	Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。
T60473	Nepinalone
	Nepinalone 是 β-tetralone 的alchilaminate 衍生物。Nepinalone 是一种口服活性止咳药，具有非阿片类止咳活性。
T3694L	Tebanicline tosylate
	Tebanicline is a potent synthetic nicotinic (non-opioid) analgesic drug. It was developed as a less toxic analogue of the potent poison dart frog-derived compound epibatidine. Like epibatidine, tebanicline showed potent analgesic activity against neuropat
T73631	(Rac)-SNC80
	(Rac)-SNC80 是SNC80 的外消旋体。SNC80 (NIH 10815) 是一种有效的，高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂，Ki 为1.78 nM，IC50为 2.73 nM。SNC80 具有抗伤害性，抗痛觉过敏和抗抑郁样作用，并可用于多种头痛症的研究。
T83709	LIH383 TFA Phe-Gly-Gly-Phe-Met-Arg-Arg-Lys-NH2
	LIH383是一种趋化因子(C-X-C motif) 受体7 (CXCR7)的多肽激动剂，属于趋化因子和阿片肽清除受体。它专一性激活CXCR7 (EC50 = 0.61 nM)，在3 µM浓度时，相比μ-、δ-、κ-阿片受体以及诺氨酸阿片肽（NOP）受体的β-arrestin招募实验中表现出高选择性。LIH383（3 µM）通过阻止U87-ACKR3细胞中，由非选择性阿片受体激动剂dynorphin A诱导的CXCR7对阿片肽的摄取，发挥作用。

化合物

Opiranserin hydrochloride

Cat.No: T9833

Target: P2X Receptor, GlyT, 5-HT Receptor

Flupirtine maleate

Cat.No: T6504

Synonym: Katadolon maleate,氟吡啶马来酸,马来酸氟吡汀

Target: Potassium Channel, NMDAR, iGluR

Ziconotide Acetate (107452-89-1 free base)

Cat.No: TP1559L

Synonym: 醋酸齐考诺肽,Prialt,Ziconotide Acetate

Target: Calcium Channel

Cat.No: T16399

Target: P2X Receptor, GlyT, 5-HT Receptor

Tebanicline hydrochloride

Cat.No: T3720

Synonym: 替巴克兰盐酸盐,ABT-594 hydrochloride,Ebanicline hydrochloride

Target: AChR

Vocacapsaicin hydrochloride

Cat.No: T39349

Synonym: CA-008 hydrochloride

Target: TRP/TRPV Channel

Nefopam hydrochloride

Cat.No: T0470

Synonym: 盐酸奈福泮,Fenazoxine hydrochloride,Nefopam HCl

Target: Wnt/beta-catenin, Sodium Channel

AT-121 hydrochloride

Cat.No: T39529

Target: Opioid Receptor

Cat.No: T8414

Synonym: Snc-80,SNC80,NIH 10815

Target: Opioid Receptor

Cat.No: T37610

Target: Opioid Receptor

Cat.No: T27253

Cat.No: T23972

Synonym: DDD 028,DDD-028

Cat.No: T34784

Synonym: SB-205607 dihydrobromide,SB 205607 dihydrobromide,SB205607 dihydrobromide,TAN-67,TAN 67

Levallorphan tartrate

Cat.No: T25690

Synonym: Lorfan

Enkephalin-leu, ala(2)-ser(6)-

Cat.No: T31631

Synonym: DALES,2-Ala-6-ser-leu-enkephalin

Cat.No: T26475

SB 205607 dihydrobromide

Cat.No: T23313

Target: Others

Cat.No: T70503

Nepinalone hydrochloride

Cat.No: T39747

Cat.No: T39348

Synonym: CA-008,Vocacapsaicin

Lappaconitine HCl

Cat.No: T2806L

Synonym: Lappaconitine hydrochloride

Cat.No: T69422

Gaboxadol hydrobromide

Cat.No: T68933

Naltrindole hydrochloride

Cat.No: T12169

Target: Opioid Receptor

Cat.No: T27363

Synonym: FR-64822,FR64822

Bicifadine free base

Cat.No: T71772

Cat.No: T38192

Target: Others

Cat.No: T60473

Tebanicline tosylate

Cat.No: T3694L

Cat.No: T73631

Cat.No: T83709

Synonym: Phe-Gly-Gly-Phe-Met-Arg-Arg-Lys-NH2

Cat. No.	Product Name	Target	Signaling Pathways
T2870	Matrine Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine	Mitophagy; Ferroptosis; Opioid Receptor; Autophagy	Apoptosis; Autophagy; Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Matrine (Vegard) 是一种从槐属植物中分离出来的生物碱，可作为一种κ阿片受体激动剂，有抗肿瘤活性。
T23306	Salvinorin A	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Salvinorin A 是一种非含氮 κ-opioid 样物质选择性激动剂。

天然产物

Cat.No: T2870

Synonym: Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine

Target: Mitophagy, Ferroptosis, Opioid Receptor, Autophagy

Cat.No: T23306

Target: Opioid Receptor

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