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374

抑制剂 & 化合物

19

天然产物

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Cat. No. Product Name Target Signaling Pathways
T12314 Opioid receptor modulator 1

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Opioid receptor modulator 1 is a modulator of opioid receptor.
T62767 Mu opioid receptor antagonist 3

Mu opioid receptor antagonist 3 (compound 26) 是一种有效的、选择性的、能透过血脑屏障渗透性的μ 阿片受体 (MOR) 拮抗剂 (Ki: 0.24 nM, EC50: 0.54 nM)。Mu opioid receptor antagonist 2 对吗啡表现出明显的中枢神经系统拮抗活性,诱发戒断症状比 Naloxone 小。Mu opioid receptor antagonist 2 能够用于研究阿片类药物使用障碍 (OUD)。
T62025 μ opioid receptor agonist 2

μ opioid receptor agonist 2 (Compound H-3)是一种MOR 受体激动剂,可用于疼痛及疼痛相关疾病的研究。
T79430 μ opioid receptor agonist 3

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
μopioid receptor agonist3 (compound 20) 是高效的μOR激动剂,其EC50 值为0.87 nM。该化合物在疼痛和神经精神适应症研究中具备潜在应用价值。
T62268 μ opioid receptor agonist 1

μ opioid receptor agonist 1 (Compound H-1a)是一种光学纯的氧杂环取代吡咯并吡唑衍生物,也是一种 MOR 受体激动剂,能够用于研究疼痛及疼痛相关疾病。
T8991 BMS986187

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
BMS986187 是一种有效的δ-阿片受体选择性正变构调节剂 (PAM),其 EC50= 0.03 μM,pKB= 6.02 (~1 μM)。BMS986187 对 μ 受体无明显 PAM 活性 (EC50=3 μM)。
T4691 Asimadoline hydrochloride

EMD-61753 hydrochloride,阿西马朵林盐酸盐

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Asimadoline hydrochloride (EMD-61753 hydrochloride) 是一种 κ-阿片(κ-opioid)受体激动剂,对豚鼠和人重组 κ-opioid 的 IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛,具有外周抗炎作用,并有用于肠易激综合征的研究潜力。
T9459 GR103545

Others Others
GR103545 是 κ-阿片受体的选择性激动剂,它是一种放射性示踪剂,可以用作体内成像。
T62673 Mu opioid receptor antagonist 5

Mu opioid receptor antagonist 5 (compound NAP) 是一种选择性的、能够透过血脑屏障的 μ 阿片受体 (MOR) 拮抗剂 (EC50: 1.14 nM, Ki: 0.37 nM)。Mu opioid receptor antagonist 5 能够用于研究阿片类药物使用障碍 (OUD)。
T7748 Dermorphin TFA

皮啡肽三氟乙酸盐

Others; Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others
Dermorphin TFA 是在两栖类皮肤中发现的天然七肽,是 μ-阿片受体激动剂,可用于抑制神经痛。
T4351 DAMGO

Dagol,DAGO,RX-783006

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
DAMGO (DAGO) 是一种阿片受体激动剂,Kd 值为 3.46 nM。它能够影响啮齿动物的运动活动,可作为镇痛剂。
T61901 σ1 Receptor/μ Opioid receptor modulator 1

σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) 是一种有效的σ1受体拮抗剂(Ki= 1.86 nM)和μ阿片受体激动剂(Ki=2.1 nM)。σ1 Receptor/μ Opioid receptor modulator 1 具体有效的镇痛活性,可用于神经性疼痛的研究。
T79431 Mu opioid receptor antagonist 7

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Muopioid receptorantagonist 7 (compound 24) 是一种有效的CNS渗透性μOR (μ-阿片受体)拮抗剂,具有29 ± 3.0 nM的IC50。该化合物可用于研究疼痛和阿片类药物使用障碍。
T62766 Mu opioid receptor antagonist 2

Mu opioid receptor antagonist 2 (compound 25) 是一种有效的、选择性的、能透过血脑屏障渗透性的μ 阿片受体 (MOR) 拮抗剂 (Ki: 0.37 nM, EC50: 0.44 nM)。Mu opioid receptor antagonist 2 对吗啡表现出明显的中枢神经系统拮抗活性,诱发戒断症状比 Naloxone 小。Mu opioid receptor antagonist 2 能够用于研究阿片类药物使用障碍 (OUD)。
T62768 Mu opioid receptor antagonist 4

Mu opioid receptor antagonist 4 (compound 31) 是一种有效的、选择性的、能透过血脑屏障渗透性的μ 阿片受体 (MOR) 拮抗剂 (Ki: 0.38 nM, EC50: 0.38 nM)。Mu opioid receptor antagonist 2 对吗啡表现出明显的中枢神经系统拮抗活性,诱发戒断症状比 Naloxone 小。Mu opioid receptor antagonist 2 能够用于研究阿片类药物使用障碍 (OUD)。
TP1832 Gluten Exorphin C

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Gluten exorphin C 是来源于谷朊粉的阿片肽。在 GPI 和 MVD 检测中,抑制 μ 阿片和 δ 阿片活性,IC50值分别为 40 和13.5 μM。
T0918 Trimebutine

曲美布汀,Mebutin

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Trimebutine (Mebutin) 是阿片受体激动剂,有抗毒蕈碱活性。它是解痉剂,可调节肠道和结肠运动,并通过抗毒蕈碱和弱μ-阿片受体激动剂作用缓解腹痛。
T1242 Alvimopan

爱维莫潘

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Alvimopan (LY 246736) 是一种选择性和竞争性 μ 阿片受体拮抗剂,IC50值为 1.7 nM。它存在于肌间和黏膜下神经元以及人体肠道固有层的免疫细胞中,可用于术后肠梗阻的研究。
TP1071 Nociceptin

Orphanin FQ,孤菲肽

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Nociceptin (Orphanin FQ) 是一种 17 个氨基酸的多肽,是 nociceptin 受体的内源性配体,具有缓解疼痛的作用。
T13414 ZT 52656A hydrochloride

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
ZT 52656A hydrochloride 是一种 kappa 阿片样物质的选择性激动剂,用于预防或减轻眼部疼痛。
T4386 PZM21

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
PZM21 是一种有效的选择性 μ 阿片受体激动剂,EC50值为 1.8 nM。
T8992 BMS986188

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
BMS986188 是一种新型的强效选择性正向变构调节剂,用于 δ-阿片受体。
T4407 SR17018

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
SR17018 是一种 μ-阿片受体 (MOR) 激动剂,与 GTPγS 结合,EC50 为 97 nM。
T7218 Endomorphin 2

内吗啡肽 2

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Endomorphin 2 是一种高亲和力和选择性的 μ-阿片受体激动剂,对 kappa3 结合位点具有合理的亲和力 ,Ki 为 20 到 30 nM 之间。
T2071 MCOPPB triHydrochloride

MCOPPB trihydrochlride,MCOPPB 3HCl

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
MCOPPB triHydrochloride (MCOPPB 3HCl) 是一种伤害感受肽受体激动剂,pKi 为10.07。
TQ0267 Endomorphin 1

内吗啡肽 1,Endomorphin-1

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Endomorphin 1 是一种高亲和力和选择性的 μ-阿片受体激动剂,对 kappa3 结合位点具有合理的亲和力 ,Ki 为 20 到 30 nM 之间。
T1197 Trimebutine maleate

Debridat,Polibutin,马来酸曲美布汀

Calcium Channel; Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience
Trimebutine maleate (Polibutin) 是一种外周 μ、δ 和 kappa 阿片受体激动剂,用作治疗慢性和急性腹痛的解痉药物。
T5167 Cebranopadol

西博帕多,GRT6005

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Cebranopadol (GRT6005) 是镇痛 NOP 和阿片受体激动剂,对人 NOP、μ-阿片 (MOP)、κ-阿片 (KOP) 和 δ-阿片 (DOP) 受体的 Ki 值分别为 0.9、0.7、2.6 和 18 nM。
TQ0091 LY2795050

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
LY2795050 是一种新型特异性 κ-阿片受体拮抗剂,IC50为0.72 nM。
TP1905 BW-180C

(D-丙2,D-亮5)-脑啡肽,DADLE

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
BW-180C (DADLE) 是水溶性的多肽类δ-阿片受体激动剂,也对 μ-阿片受体显示活性,在体内表现出镇痛活性。
T6414 Bisacodyl

比沙可啶,Fenilaxan,Dulcolax,Brocalax

Others Others
Bisacodyl (Fenilaxan) 是刺激性缓泻剂,可直接作用于结肠以产生排便。它能够直接激活结肠巨噬细胞来增加 PGE2的分泌。PGE2充当旁分泌因子并减少结肠中 AQP3 的表达,抑制水从腔向血管一侧的转移,进而产生通便作用。
T26869 BMS-986122

BMS 986122

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
BMS-986122 (BMS 986122) 是选择性 μ 阿片受体正变构调节剂,可增加 β-抑制蛋白募集、腺苷酸环化酶抑制和 G 蛋白活化的作用,还增强 DAMGO 介导的 [35S]GTPγS 在小鼠脑膜中的结合。
TP1367 [D-Ala2]leucine-enkephalin

(D-ALA2)-亮氨酸脑啡肽

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
[D-Ala2]leucine-enkephalin 是 δ 阿片类激动剂,是能长效抗降解的亮氨酸脑非肽,可用于研究 δ 阿片受体的信号通路。
T14551 Bevenopran

CB-5945,ADL-5945

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Bevenopran (CB-5945) is a peripheral antagonist of μ-opioid receptor and can be used in studies about the treatment of opioid-induced bowel dysfunction.
TQ0082 Aticaprant

LY-2456302,CERC-501

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Aticaprant (LY-2456302) 是一种有效的中枢渗透性 kappa-阿片受体拮抗剂,Ki 值为 0.807 nM。
T15799 LY2940094

LY-2940094

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
LY2940094 (LY-2940094) 是一种口服有效的选择性 NOP 受体拮抗剂,可降低动物模型的自身给药酒精依赖,对 NOP 受体具有高亲和力,Ki 为 0.105 nM,和拮抗活力,Kb 为 0.166 nM。
T7639 Deltorphin 2

Deltorphin 2(TFA),[D-Ala2]-Deltorphin II

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Deltorphin 2 ([D-Ala2]-Deltorphin II) 是一种选择性的 δ 阿片受体肽激动剂,IC50 为 1 nM。
T6175 ADL-5859

ADL5859 Hydrochloride,ADL5859 HCl

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
ADL-5859 (ADL5859 Hydrochloride) 是δ-阿片受体选择性激动剂,Ki 为0.8 nM,对阿片受体 κ 和 μ 具有选择性。
T7637 Deltorphin I

Deltorphin 1,Deltorphin I(TFA),Deltorphin C

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Deltorphin I 是 δ-阿片受体的激动剂。
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。
T3996 Dapiprazole Hydrochloride

盐酸达哌唑,Glamidolo Hydrochloride,Reversil Hydrochloride

Adrenergic Receptor GPCR/G Protein; Neuroscience
Dapiprazole Hydrochloride (Glamidolo Hydrochloride) 是 α-adrenergic 阻断剂的药物。
T14835 BTRX-335140

CYM-53093

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
BTRX-335140 (CYM-53093) 是一种有效的选择性口服活性 κ 阿片受体 (KOR) 拮抗剂,对 κOR、μOR 和 δOR 具有拮抗活性,IC50 值分别为 0.8、110 和 6500 nM。它可以很好地分布到 CNS 中,在大鼠中具有良好的体外吸收、分布、代谢、排泄和毒性以及体内药代动力学特征。
T5158 N-Desmethylclozapine

N-去甲基氯氮平,Desmethylclozapine,Normethylclozapine,Norclozapine

Virus Protease; Dopamine Receptor; 5-HT Receptor; Opioid Receptor; AChR; Drug Metabolite Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
N-Desmethylclozapine (Desmethylclozapine) 是非典型抗精神病药 Clozapine 的主要活性代谢产物。它是血清素受体亚型 5-HT2C 的拮抗剂,IC50值为7.1 nM。 它也是多巴胺 D4 受体的拮抗剂和δ-阿片受体的激动剂。
TP2036L DPDPE TFA (88373-73-3 free base)

DPDPE TFA

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
DPDPE TFA 是选择性 δ-阿片受体激动剂肽,在体内具有镇痛作用。
T4633 Asimadoline

EMD-61753,阿西马朵林

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Asimadoline (EMD-61753) 是一种 κ-阿片(κ-opioid)受体激动剂,对豚鼠和人重组 κ-opioid 的IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛,具有外周抗炎作用,并有用于肠易激综合征的研究潜力。
T7211 Tyr-Gly-Gly-Phe-Met-OH

Methionine enkephalin,蛋氨酸脑啡肽,Met-Enkephalin,[MET5]脑啡肽

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Tyr-Gly-Gly-Phe-Met-OH (Met-Enkephalin) 是天然存在的内源性阿片肽、metenkephalin 和 zeta-和 delta-阿片受体激动剂的合成形式,是 mu-阿片受体激动剂,具有潜在的镇痛、神经调节、免疫调节、抗炎、抗肿瘤作用以及镇痛、抗抑郁和胃肠运动调节活性。
T7173 [Leu5]-Enkephalin

亮氨酸脑啡肽,Leucine enkephalin,Leucyl-enkephalin,Leu-enkephalin

Opioid Receptor; Endogenous Metabolite Endocrinology/Hormones; GPCR/G Protein; Metabolism; Neuroscience
[Leu5]-Enkephalin (Leu-enkephalin) 是一种参与伤害感受的内源性神经肽,是 δ-阿片和 μ-阿片受体的激动剂,Ki 值分别为 4.0 和 3.4 nM
T7404 Dermorphin

皮啡肽

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Dermorphin 是在两栖类皮肤中发现的天然七肽,是 μ-阿片受体激动剂,可用于抑制神经痛。
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。
T21422 Methylnaltrexone bromide

Relistor,MOA-728,MOA 728,Methylnaltrexone,溴化甲基纳曲酮,MOA728

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Methylnaltrexone bromide (MOA-728) 是纳曲酮的四元衍生物,是可口服的外周作用 μ 阿片拮抗剂。它穿越血脑屏障的能力有限,可在胃肠道组织中发挥作用。

化合物

Opioid receptor modulator 1
Cat.No: T12314
Synonym:
Target: Opioid Receptor
Mu opioid receptor antagonist 3
Cat.No: T62767
Synonym:
Target:
μ opioid receptor agonist 2
Cat.No: T62025
Synonym:
Target:
μ opioid receptor agonist 3
Cat.No: T79430
Synonym:
Target: Opioid Receptor
μ opioid receptor agonist 1
Cat.No: T62268
Synonym:
Target:
BMS986187
Cat.No: T8991
Synonym:
Target: Opioid Receptor
Asimadoline hydrochloride
Cat.No: T4691
Synonym: EMD-61753 hydrochloride,阿西马朵林盐酸盐
Target: Opioid Receptor
GR103545
Cat.No: T9459
Synonym:
Target: Others
Mu opioid receptor antagonist 5
Cat.No: T62673
Synonym:
Target:
Dermorphin TFA
Cat.No: T7748
Synonym: 皮啡肽三氟乙酸盐
Target: Others, Opioid Receptor
DAMGO
Cat.No: T4351
Synonym: Dagol,DAGO,RX-783006
Target: Opioid Receptor
σ1 Receptor/μ Opioid receptor modulator 1
Cat.No: T61901
Synonym:
Target:
Mu opioid receptor antagonist 7
Cat.No: T79431
Synonym:
Target: Opioid Receptor
Mu opioid receptor antagonist 2
Cat.No: T62766
Synonym:
Target:
Mu opioid receptor antagonist 4
Cat.No: T62768
Synonym:
Target:
Gluten Exorphin C
Cat.No: TP1832
Synonym:
Target: Opioid Receptor
Trimebutine
Cat.No: T0918
Synonym: 曲美布汀,Mebutin
Target: Opioid Receptor
Alvimopan
Cat.No: T1242
Synonym: 爱维莫潘
Target: Opioid Receptor
Nociceptin
Cat.No: TP1071
Synonym: Orphanin FQ,孤菲肽
Target: Opioid Receptor
ZT 52656A hydrochloride
Cat.No: T13414
Synonym:
Target: Opioid Receptor
PZM21
Cat.No: T4386
Synonym:
Target: Opioid Receptor
BMS986188
Cat.No: T8992
Synonym:
Target: Opioid Receptor
SR17018
Cat.No: T4407
Synonym:
Target: Opioid Receptor
Endomorphin 2
Cat.No: T7218
Synonym: 内吗啡肽 2
Target: Opioid Receptor
MCOPPB triHydrochloride
Cat.No: T2071
Synonym: MCOPPB trihydrochlride,MCOPPB 3HCl
Target: Opioid Receptor
Endomorphin 1
Cat.No: TQ0267
Synonym: 内吗啡肽 1,Endomorphin-1
Target: Opioid Receptor
Trimebutine maleate
Cat.No: T1197
Synonym: Debridat,Polibutin,马来酸曲美布汀
Target: Calcium Channel, Opioid Receptor
Cebranopadol
Cat.No: T5167
Synonym: 西博帕多,GRT6005
Target: Opioid Receptor
LY2795050
Cat.No: TQ0091
Synonym:
Target: Opioid Receptor
BW-180C
Cat.No: TP1905
Synonym: (D-丙2,D-亮5)-脑啡肽,DADLE
Target: Opioid Receptor
Bisacodyl
Cat.No: T6414
Synonym: 比沙可啶,Fenilaxan,Dulcolax,Brocalax
Target: Others
BMS-986122
Cat.No: T26869
Synonym: BMS 986122
Target: Opioid Receptor
[D-Ala2]leucine-enkephalin
Cat.No: TP1367
Synonym: (D-ALA2)-亮氨酸脑啡肽
Target: Opioid Receptor
Bevenopran
Cat.No: T14551
Synonym: CB-5945,ADL-5945
Target: Opioid Receptor
Aticaprant
Cat.No: TQ0082
Synonym: LY-2456302,CERC-501
Target: Opioid Receptor
LY2940094
Cat.No: T15799
Synonym: LY-2940094
Target: Opioid Receptor
Deltorphin 2
Cat.No: T7639
Synonym: Deltorphin 2(TFA),[D-Ala2]-Deltorphin II
Target: Opioid Receptor
ADL-5859
Cat.No: T6175
Synonym: ADL5859 Hydrochloride,ADL5859 HCl
Target: Opioid Receptor
Deltorphin I
Cat.No: T7637
Synonym: Deltorphin 1,Deltorphin I(TFA),Deltorphin C
Target: Opioid Receptor
Opiranserin hydrochloride
Cat.No: T9833
Synonym:
Target: P2X Receptor, GlyT, 5-HT Receptor
Dapiprazole Hydrochloride
Cat.No: T3996
Synonym: 盐酸达哌唑,Glamidolo Hydrochloride,Reversil Hydrochloride
Target: Adrenergic Receptor
BTRX-335140
Cat.No: T14835
Synonym: CYM-53093
Target: Opioid Receptor
N-Desmethylclozapine
Cat.No: T5158
Synonym: N-去甲基氯氮平,Desmethylclozapine,Normethylclozapine,Norclozapine
Target: Virus Protease, Dopamine Receptor, 5-HT Receptor, Opioid Receptor, AChR, Drug Metabolite
DPDPE TFA (88373-73-3 free base)
Cat.No: TP2036L
Synonym: DPDPE TFA
Target: Opioid Receptor
Asimadoline
Cat.No: T4633
Synonym: EMD-61753,阿西马朵林
Target: Opioid Receptor
Tyr-Gly-Gly-Phe-Met-OH
Cat.No: T7211
Synonym: Methionine enkephalin,蛋氨酸脑啡肽,Met-Enkephalin,[MET5]脑啡肽
Target: Opioid Receptor
[Leu5]-Enkephalin
Cat.No: T7173
Synonym: 亮氨酸脑啡肽,Leucine enkephalin,Leucyl-enkephalin,Leu-enkephalin
Target: Opioid Receptor, Endogenous Metabolite
Dermorphin
Cat.No: T7404
Synonym: 皮啡肽
Target: Opioid 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
Methylnaltrexone bromide
Cat.No: T21422
Synonym: Relistor,MOA-728,MOA 728,Methylnaltrexone,溴化甲基纳曲酮,MOA728
Target: Opioid Receptor
Cat. No. Product Name Target Signaling Pathways
T6S1010 Allomatrine

槐定碱,别苦参碱

Others Others
Allomatrine 是一种来源槐花树皮的生物碱。它能够激活 κ-阿片受体,进而产生缓解疼痛的作用。
T5S0581 Sec-O-Glucosylhamaudol

亥茅酚苷,Hamaudol 3-glucoside

Others; Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others
Sec-O-Glucosylhamaudol (Hamaudol 3-glucoside) 是从滨海前胡中分离得到的一种天然产物,能够降低 μ 阿片受体的蛋白水平,可用于缓解疼痛的研究。它通过调节脂多糖刺激的 RAW264.7 细胞系中的 p38 丝裂原活化蛋白激酶具有抗炎作用。
T2726 Sinomenine

Cucoline,Kukoline,青藤碱

Apoptosis; Others; NF-κB; Opioid Receptor; Autophagy Apoptosis; Autophagy; Endocrinology/Hormones; GPCR/G Protein; Neuroscience; NF-κB; Others
Sinomenine (Kukoline) 是来自汉防己的一种生物碱,是 μ 阿片受体激活剂,也是NF-κB 活化的阻断剂。
T5S2360 Corydaline

Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline

P450; Virus Protease; Opioid Receptor; AChE Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
Corydaline (Corydalin) 是从 Corydalis yanhusuo 提取的一种异喹啉生物碱,是一种新型促动力植物药的主要活性成分之一。它促进胃排空和小肠转运,促进胃的调节,具有抗乙酰胆碱酯酶、抗过敏和镇痛活性。
T2921 Sinomenine hydrochloride

盐酸青藤碱,Sabianine A hydrochloride,Cucoline hydrochloride,Kukoline hydrochloride

Apoptosis; NF-κB; Opioid Receptor; Autophagy Apoptosis; Autophagy; Endocrinology/Hormones; GPCR/G Protein; Neuroscience; NF-κB
Sinomenine hydrochloride (Kukoline hydrochloride) 是来自汉防己的一种生物碱,是NF-κB 活化的阻断剂。Sinomenine 也是一种 μ 阿片受体激活剂。
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。
TN1308 6-Hydroxyflavanone

Others; Lipoxygenase; COX; GABA Receptor Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; Others
6-Hydroxyflavanone 是从菖蒲叶中提取分离,通过靶向环氧合酶-2(COX-2),5-脂氧合酶(5-LOX)以及阿片类药物和 GABA-A 受体从而具有抗炎和抗神经性疼痛活性。6-Hydroxyflavanone 在链脲佐菌素诱导的糖尿病神经病变模型中具有抗伤害感受特性。
T2S2362 Dehydrocorydaline nitrate

去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱

BCL; Others; PARP; p38 MAPK; Caspase; Parasite; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Others; Proteases/Proteasome
Dehydrocorydaline nitrate 是生物碱。Dehydrocorydaline 调节 Bax,Bcl-2蛋白表达,激活 caspase-7,caspase-8,并使 PARP 失活。它能增强 p38 MAPK 活化,具有抗炎、抗癌、抗疟疾等功效。
T3417 Amentoflavone

Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物,有抗炎、抗氧化和神经保护等作用。
T5S0754 Isoquercetin

3-Glucosylquercetin,Hirsutrin,Isoquercitrin,异槲皮苷,Quercetin 3-o-glucopyranoside,槲皮素-3-葡萄糖苷

NF-κB; Wnt/beta-catenin; NO Synthase Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; Stem Cells
Isoquercetin (3-Glucosylquercetin) 是天然存在的多酚,具有抗氧化,抗增殖和抗炎特性。它通过调节核因子-κB 转录调节系统调节一氧化氮合酶 2 的表达。它通过 Nrf2/ARE 抗氧化剂信号传导途径减轻乙醇诱导的肝毒性,氧化应激和炎症反应。它具有高生物利用度和低毒性,是预防糖尿病妊娠出生缺陷的有希望的候选药物。
TN3367 Akuammidine

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Akuammidine shows anti-inflammatory and anti-asthmatic properties, it has opioid analgesic activity, it shows a preference for mu-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 microM at mu-, delta- and kappa-opioid binding sites, respectively.
T76027 β-Endorphin, equine TFA

β-Endorphin, equine TFA,是具备强效亲和力于μ和δ阿片受体(μ/δ opioid receptors)的内源性阿片类多肽,主要功能包括止痛。
TN1890 Lupeol acetate

Others; TNF; NOS Apoptosis; Immunology/Inflammation; Others
Lupeol acetate possesses antinociceptive, antifertility, and anti-inflammatory properties, the effect probably involves the opioid system, as indicated by the complete blockade of the opioid antagonist naloxone.
T13433 β-Endorphin, human

Others Others
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus,and is an agonist of opioid receptor.
TN3368 Akuammigine

Opioid Receptor; Adrenergic Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding pA2 values of 4.68. Akuammidine also shows a preference for mu-opioid binding sites with Ki val
TN4613 (-)-N-methylcoclaurine

N-Methylcoclaurine

Others Others
N-Methylcoclaurine shows binding affinities for the ĸ opioid receptor with the equilibrium dissociation constant (Ki) value of 0.9 ± 0.1 uM. N-methylcoclaurine also shows promising butyrylcholinesterase inhibition activities, with the IC50 value of 1
T83913 Mitraciliatine

Mitraciliatine是一种在M. speciosa(泰国称为Kratom)中发现的生物碱,是μ-阿片受体(MOR)部分激动剂和κ-阿片受体(KOR)激动剂。该化合物对MOR和KOR具有选择性,与δ-阿片受体(DOR; EC50s分别为228, 218, 和 >1,000 nM,针对小鼠受体在GTPγS结合实验中的表现)。Mitraciliatine(100 nmol/动物,脑室内注射)在小鼠的热水尾部缩回实验中延长了撤回潜伏期,这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同,Mitraciliatine不会诱发过度活动或呼吸抑制。
TN4064 Flavoglaucin

Phosphatase; IL Receptor; TNF; NOS; NF-κB; COX; Nrf2; Prostaglandin Receptor; Autophagy Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
Flavoglaucin exhibits significant inhibitory effects on PTP1B, the IC50 value of 13.4, micrometer; it also shows good binding affinity for human opioid or cannabinoid receptors. Flavoglaucin appears to be an antitumor promoter, it also has anti-inflammato

天然产物

Allomatrine
Cat.No: T6S1010
Synonym: 槐定碱,别苦参碱
Target: Others
Sec-O-Glucosylhamaudol
Cat.No: T5S0581
Synonym: 亥茅酚苷,Hamaudol 3-glucoside
Target: Others, Opioid Receptor
Sinomenine
Cat.No: T2726
Synonym: Cucoline,Kukoline,青藤碱
Target: Apoptosis, Others, NF-κB, Opioid Receptor, Autophagy
Corydaline
Cat.No: T5S2360
Synonym: Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline
Target: P450, Virus Protease, Opioid Receptor, AChE
Sinomenine hydrochloride
Cat.No: T2921
Synonym: 盐酸青藤碱,Sabianine A hydrochloride,Cucoline hydrochloride,Kukoline hydrochloride
Target: Apoptosis, NF-κB, Opioid Receptor, Autophagy
Matrine
Cat.No: T2870
Synonym: Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine
Target: Mitophagy, Ferroptosis, Opioid Receptor, Autophagy
Salvinorin A
Cat.No: T23306
Synonym:
Target: Opioid Receptor
6-Hydroxyflavanone
Cat.No: TN1308
Synonym:
Target: Others, Lipoxygenase, COX, GABA Receptor
Dehydrocorydaline nitrate
Cat.No: T2S2362
Synonym: 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱
Target: BCL, Others, PARP, p38 MAPK, Caspase, Parasite, Autophagy
Amentoflavone
Cat.No: T3417
Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin
Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal
Isoquercetin
Cat.No: T5S0754
Synonym: 3-Glucosylquercetin,Hirsutrin,Isoquercitrin,异槲皮苷,Quercetin 3-o-glucopyranoside,槲皮素-3-葡萄糖苷
Target: NF-κB, Wnt/beta-catenin, NO Synthase
Akuammidine
Cat.No: TN3367
Synonym:
Target: Opioid Receptor
β-Endorphin, equine TFA
Cat.No: T76027
Synonym:
Target:
Lupeol acetate
Cat.No: TN1890
Synonym:
Target: Others, TNF, NOS
β-Endorphin, human
Cat.No: T13433
Synonym:
Target: Others
Akuammigine
Cat.No: TN3368
Synonym:
Target: Opioid Receptor, Adrenergic Receptor
(-)-N-methylcoclaurine
Cat.No: TN4613
Synonym: N-Methylcoclaurine
Target: Others
Mitraciliatine
Cat.No: T83913
Synonym:
Target:
Flavoglaucin
Cat.No: TN4064
Synonym:
Target: Phosphatase, IL Receptor, TNF, NOS, NF-κB, COX, Nrf2, Prostaglandin Receptor, Autophagy
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