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38

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
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)。
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。
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)。
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)。
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。
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。
T27667 JNJ-20788560

JNJ 20788560

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
JNJ-20788560 是一种δ阿片受体(DOR)激动剂,具有镇痛活性。它对 DOR 的选择性高于μ阿片受体(MOR)。
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。
T31081 CP-866087

CP 866087,UNII-MDH21334PI,CP-866,087,CP866087

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
CP-866087 是一种新型、有效和选择性的μ阿片受体拮抗剂,用于研究女性性功能障碍。
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。
T50091 1,1'-(Octane-1,8-diyl)diguanidine dihydrochloride

1-(8-carbamimidamidooctyl)guanidine dihydrochloride

Others Others
1,1'-(Octane-1,8-diyl)diguanidine dihydrochloride 是一种合成的阿片肽,来源于天然阿片肽脑啡肽。它是μ-阿片受体(MOR)的高效激动剂,Ki 为0.14 nM,是一种有效的MOR 激动剂。
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。
T10593 BPR1M97

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
BPR1M97 是一种具有血脑屏障渗透性和有效性的 mu 阿片受体(MOP)和神经肽-啡肽 FQ(NOP)受体激动剂,对 MOP 的 Kis 值为1.8 nM,对 NOP 的Kis 值为 4.2 nM。BPR1M97 具有抗伤害作用和抗痛觉作用。
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。
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。
T7306 Valorphin

Valorphin TFAsalt

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Valorphin (Valorphin TFAsalt) 是内源性血红蛋白 β 链第 33-39 位氨基酸残基,具有阿片类镇痛活性,与大鼠 mu-阿片受体结合,IC50 为 14 nM。它有抗肿瘤活性,也可用于缓解疼痛的研究。
T25194 BW 443C

BW443C,BW-443C,Tyr-arg-gly-(4-nitro-phe)-pro-NH2

BW 443C is a selective agonist of mu-opioid receptor.
T71189 RX 809055AX

RX 809055AX is a long lasting opioid antagonist at mu and delta receptors.
T26918 BU08028

BU 08028,BU-08028

BU08028 is a mu opioid peptide (MOP) receptor and nociceptin-orphanin FQ peptide (NOP) receptor agonist.
T70730 Oxycodegol phosphate

Oxycodegol phosphate is a mu​-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain
T1242L Alvimopan monohydrate

Alvimopan monohydrate is a mu-opioid receptor antagonist that intended for the treatment of constipation in patients who take opiates for pain.
T69121 Oxpheneridine

Oxpheneridine is a mu opioid receptor agonist that possesses the spasmolytic activity and acts as a narcotic analgesic.
T10926L CYT-1010 hydrochloride

Others Others
CYT-1010 hydrochloride is an mu-opioid receptor agonist. The EC50 for β-arrestin recruitment and cAMP production inhibition were 13.1 nM and 0.0053 nM, respectively.
T60415 DS34942424

DS34942424 是一种没有μ 阿片受体激动剂活性的口服强效镇痛剂。
T71225 Oxicodegol HCl

Oxicodegol HCl is a mu​-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain
T71224 Oxicodegol trifluoroacetate

Oxicodegol trifluoroacetate is a mu​-opioid agonist used in the treatment of Moderate to Severe Chronic Low Back Pain
T10926 CYT-1010

Others Others
CYT-1010 is an mu-opioid receptor agonist. The EC50 for the inhibition of β-arrestin recruitment and cAMP production is 13.1 nM and 0.0053 nM, respectively.
T62722 SC13

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。
T27027 CJ-15208

CJ15,208,CJ-15,208,CJ 15,208.c[Phe-D-Pro-Phe-Trp]

CJ-15208 is a potent and selective κ-opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502 (IC50 are 47 nM for kappa, 260 nM for mu, and 2,600 nM for delta respectly). In the electrically-stimulated twitch response assay of rabbit vas de
T40845 Methylnaltrexone iodide

Naltrexonium methiodide,碘化甲基纳曲酮; 碘甲纳曲酮

Methylnaltrexone iodide, a quaternary derivative of Naltrexone, is an orally active and selective antagonist of the mu-opioid receptor. It acts peripherally in the gastrointestinal tract to antagonize the receptor. Furthermore, Methylnaltrexone iodide exhibits limited permeability across the blood-brain barrier.
T4411 DAMGO TFA (78123-71-4(Free base))

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
DAMGO TFA (78123-71-4(Free base)) 是Mu-opioid 受体的强效选择性激动剂。它也是镇痛药。它刺激钙激活的腺苷酸环化酶相关 cAMP 的产生。通过 TGF-beta1 表达趋化因子和趋化因子受体。增加老鼠的食物摄入量。
T75916 Dynorphin A TFA

Dynorphin A TFA, 作为一种内源性阿片肽,主要在中枢神经系统(CNS)中发挥抑制性神经传导的作用。该化合物不仅是kappa阿片受体(KOR)的高效激动剂,还能激活其他阿片受体,包括mu(MOR)和delta(DOR)。Dynorphin A TFA具有诱导神经元死亡的能力,因此在神经系统疾病的研究中具有应用价值。
T27934 LY255582

LY-255582,LY 255582

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
LY255582 是一种具有选择性的中枢活性阿片受体拮抗剂,对 mu、delta 和 kappa 受体具有高亲和力 ,Ki 分别为 0.4 nM、5.2、2.0 nM。LY255582 可以抑制饮食相关的中脑边缘多巴胺水平的增加,并减少食物摄入的消耗。LY255582 常用于对肥胖的研究。LY255582是用于阿片受体介导的细胞信号传导研究的潜在化合物。
T78778 D3R/MOR antagonist 1

Dopamine Receptor GPCR/G Protein; Neuroscience
D3R/MOR antagonist 1 (Compound 114) 为D3R/MOR拮抗剂,其对D3R和MOR的Ki值分别为46.5 nM和691 nM。该化合物通过MOR的部分激动作用可能具有镇痛效果,同时通过D3R的拮抗作用有助于降低阿片类药物的滥用风险。
T36722 Deltorphin II (trifluoroacetate salt)

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...
T62805 SB-612111 hydrochloride

SB-612111 hydrochloride 是一种高效的、新型的阿片受体孤儿受体 (ORL-1) 拮抗剂,对 hORL-1 具有较高的亲和力,Ki 值为 0.33 nM。SB-612111 hydrochloride 能够作用于 μ-receptor (Ki: 57.6 nM),κ-receptor (Ki: 160.5 nM) 和 δ-receptor (Ki: 2109 nM)。SB-612111 hydrochloride 能有效拮抗 Nociceptin 在急性疼痛模型中的造成的痛觉作用。

化合物

Dermorphin TFA
Cat.No: T7748
Synonym: 皮啡肽三氟乙酸盐
Target: Others, Opioid Receptor
Mu opioid receptor antagonist 3
Cat.No: T62767
Synonym:
Target:
Dermorphin
Cat.No: T7404
Synonym: 皮啡肽
Target: Opioid Receptor
Mu opioid receptor antagonist 5
Cat.No: T62673
Synonym:
Target:
Mu opioid receptor antagonist 2
Cat.No: T62766
Synonym:
Target:
Mu opioid receptor antagonist 4
Cat.No: T62768
Synonym:
Target:
Mu opioid receptor antagonist 7
Cat.No: T79431
Synonym:
Target: Opioid Receptor
Alvimopan
Cat.No: T1242
Synonym: 爱维莫潘
Target: Opioid Receptor
JNJ-20788560
Cat.No: T27667
Synonym: JNJ 20788560
Target: Opioid Receptor
Trimebutine maleate
Cat.No: T1197
Synonym: Debridat,Polibutin,马来酸曲美布汀
Target: Calcium Channel, Opioid Receptor
CP-866087
Cat.No: T31081
Synonym: CP 866087,UNII-MDH21334PI,CP-866,087,CP866087
Target: Opioid Receptor
SR17018
Cat.No: T4407
Synonym:
Target: Opioid Receptor
1,1'-(Octane-1,8-diyl)diguanidine dihydrochloride
Cat.No: T50091
Synonym: 1-(8-carbamimidamidooctyl)guanidine dihydrochloride
Target: Others
AT-121 hydrochloride
Cat.No: T39529
Synonym:
Target: Opioid Receptor
BPR1M97
Cat.No: T10593
Synonym:
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
Trimebutine
Cat.No: T0918
Synonym: 曲美布汀,Mebutin
Target: Opioid Receptor
Valorphin
Cat.No: T7306
Synonym: Valorphin TFAsalt
Target: Opioid Receptor
BW 443C
Cat.No: T25194
Synonym: BW443C,BW-443C,Tyr-arg-gly-(4-nitro-phe)-pro-NH2
Target:
RX 809055AX
Cat.No: T71189
Synonym:
Target:
BU08028
Cat.No: T26918
Synonym: BU 08028,BU-08028
Target:
Oxycodegol phosphate
Cat.No: T70730
Synonym:
Target:
Alvimopan monohydrate
Cat.No: T1242L
Synonym:
Target:
Oxpheneridine
Cat.No: T69121
Synonym:
Target:
CYT-1010 hydrochloride
Cat.No: T10926L
Synonym:
Target: Others
DS34942424
Cat.No: T60415
Synonym:
Target:
Oxicodegol HCl
Cat.No: T71225
Synonym:
Target:
Oxicodegol trifluoroacetate
Cat.No: T71224
Synonym:
Target:
CYT-1010
Cat.No: T10926
Synonym:
Target: Others
SC13
Cat.No: T62722
Synonym:
Target:
CJ-15208
Cat.No: T27027
Synonym: CJ15,208,CJ-15,208,CJ 15,208.c[Phe-D-Pro-Phe-Trp]
Target:
Methylnaltrexone iodide
Cat.No: T40845
Synonym: Naltrexonium methiodide,碘化甲基纳曲酮; 碘甲纳曲酮
Target:
DAMGO TFA (78123-71-4(Free base))
Cat.No: T4411
Synonym:
Target: Opioid Receptor
Dynorphin A TFA
Cat.No: T75916
Synonym:
Target:
LY255582
Cat.No: T27934
Synonym: LY-255582,LY 255582
Target: Opioid Receptor
D3R/MOR antagonist 1
Cat.No: T78778
Synonym:
Target: Dopamine Receptor
Deltorphin II (trifluoroacetate salt)
Cat.No: T36722
Synonym:
Target:
SB-612111 hydrochloride
Cat.No: T62805
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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.
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

天然产物

Akuammidine
Cat.No: TN3367
Synonym:
Target: Opioid Receptor
Akuammigine
Cat.No: TN3368
Synonym:
Target: Opioid Receptor, Adrenergic Receptor
TargetMol Loading
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