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Search Results for " analgesia "

36

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2524	Dexmedetomidine	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Dexmedetomidine 是选择性、具有口服活性的 α2 肾上腺素能受体激动剂，Ki=1.08 nM。它对 α1 肾上腺素受体显示出 1620 倍的选择性。它具有抗焦虑活性，可用于研究促进睡眠和缓解疼痛。
T6554	JZL 184 JZL184	Lipase	Metabolism
	JZL 184 是不可逆的、选择性的MAGL 抑制剂，对MAGL 的选择性比 FAAH 高 300 倍以上。它可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC50为 8 nM)。
T6579	Medetomidine hydrochloride MPV785,Medetomidine HCl,Domitor	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Medetomidine hydrochloride (MPV785) 是一种 α2 肾上腺素受体激动剂，能够作用于α2和α1肾上腺素受体，其Ki 分别为1.08 nM 和1750 nM。
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。
T6466	Dexmedetomidine hydrochloride Precedex,(+)-Medetomidine hydrochloride,(S)-Medetomidine hydrochloride,盐酸右美托咪定,Dexmedetomidine HCl	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Dexmedetomidine hydrochloride (Precedex) 是一种有效的、选择性的、具有口服活性的 α2 肾上腺素能受体 (α2-adrenoceptor) 激动剂，Ki=1.08 nM。它对 α1 肾上腺素受体显示出 1620 倍的选择性。它具有抗焦虑作用，可用于研究促进安定和缓解疼痛。
T1780	Parecoxib SC 69124,帕瑞昔布,Vorth-P,Valus-P	COX	Immunology/Inflammation; Neuroscience
	Parecoxib (SC 69124) 是一种有效的选择性 COX-2 抑制剂，是 Valdecoxib 的前药。
T20172L	Kyotorphin acetate	Endogenous Metabolite; Antibacterial	Metabolism; Microbiology/Virology
	Kyotorphin acetate 是一种具有镇痛活性的内源性肽，可用作阿尔茨海默病的生物标志物。
T50082	Org 25543	Chloride channel	Membrane transporter/Ion channel
	Org 25543 是一种 N-酰基氨基酸的开发，它选择性地抑制甘氨酸转运蛋白 2 以在大鼠慢性疼痛模型中产生镇痛作用。
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。
T0056	Oxeladin citrate	Others	Others
	Oxeladin citrate 是止咳剂，能够对各种病因引发咳嗽进行有效研究。
T1787	Levobupivacaine	Sodium Channel	Membrane transporter/Ion channel
	Levobupivacaine 是一种氨基酰胺类局麻药，属于n-alkylsubstituted pipecoloxylidide 家族。它是bupivacaine 的 S-对映异构体。
T34152L	Propiomazine HCl Propiomazine hydrochloride,Largon
	Propiomazine HCl is an analgesia adjunct.
T76186	Tyr-W-MIF-1
	Tyr-W-MIF-1 是一种阿片四肽，具有阿片和抗阿片活性。Tyr-W-MIF-1 可诱导镇痛。
T25675	Leucinal L-Leucinal
	Leucinal inhibits the activity of brain aminopeptidase and potentiates analgesia induced by leu-enkephalen.
T27888	LY 190388 LY190388,LY-190388
	LY 190388 is a penicillamine-containing enkephalin analog used as an mu receptor agonist with analgesia activity.
T70078	Fadolmidine
	Fadolmidine is a novel and potent alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia.
T31190	Dafphedyn
	Dafphedyn, [D-Ala2, (F5) Phe4]-dynorphin 1-13-NH2 (DAFPHEDYN) is an effective analog of strong endorphin 1-13 and produces diuretic and deep analgesia when administered intravenously in rats.
T31541	D-Kyotorphin H-L-Tyr-D-Arg-OH
	D-Kyotorphin is a synthetic neuropeptide kyotorphin analog that produces naloxone reversible analgesia.
T75919	PL-017 TFA
	PL-017 TFA 是高效、选择性的 μ 阿片受体(μopioid receptor)激动剂，具有 5.5 nM 对125I-FK 33,824 与 μ 位点结合的 IC50 值。该化合物在大鼠中展现出持久且可逆的缓解疼痛效果。
T80518	Mambalgin-3	Sodium Channel	Membrane transporter/Ion channel
	Mambalgin-3为针对酸敏感离子通道1 (ASIC1) 的抑制肽，适用于镇痛研究领域。
T32105	Cipepofol HSK3486,HSK 3486,HSK-3486
	HSK3486 is similar to propofol and is a general anesthetic, which may have therapeutic potential in insomnia, migraine, anxiety, analgesia, and other aspects.
T12970L	Solabegron HCl GW-427,353,GW427353,GW-427353,GW 427,353,GW427,353
	Solabegron (GW-427,353), is a selective agonist of β3 adrenergic receptors. In addition, Solabegron has been shown to produce visceral analgesia by releasing somatostatin from fat cells.
T68959	Fenobam hydrate
	Fenobam hydrate is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5). It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate and inhibits basal activity of mGluR5. Fenobam reduces stress-induced hyperthermia, exhibits anxiolytic-like activity, and may induce analgesia.
TP1958	PL-017 PL 017
	Selective μ opioid receptor agonist (IC50 values are 5.5 and > 10000 nM for inhibition of 125I-FK 33,824 and 125I-DADLE binding to μ and δ sites respectively). Produces naloxone-reversible analgesia, catalepsy and hyperthermia following central administra
T11038	Dibutyryl-cGMP sodium Bt2cGMP sodium	Others	Others
	Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma
T28845	SR142948A HCl SR142948A,SR 142948A,SR-142948A,SR142948A hydrochloride
	SR 142948A is a non-peptide antagonist of neurotensin receptor. SR 142948A affects the expression of c-Fos and has properties of antipsychotic agent. SR 142948A blocks hypothermia and analgesia induced by neurotensin. It blocks the increase in the concent
T37670	CAY10568
	Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported. CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists sh...
T80515	β-Endorphin (1-27) (human)	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	β-Endorphin (1-27) (human) 是一种 opioid 拮抗剂，与 μ-、δ- 及 κ-阿片受体结合，其 Kis 分别为 5.31、6.17 及 39.82 nM。该化合物还能够抑制由 β-Endorphin 及 etorphine 引起的痛觉消失。
T75840	Hemokinin 1, human TFA
	Hemokinin 1, human TFA 是选择性的速激肽神经激肽 1 (NK1) 受体完全激动剂。Hemokinin 1, human TFA 也是 NK2和 NK3受体的完全激动剂。Hemokinin 1, human TFA 可以产生非阿片样物质的缓解疼痛作用。
T81763	MOR agonist-3
	MOR Agonist-3 (Compound 84) 是一种双重作用化合物，具有D3R/MOR拮抗活性（Ki值为55.2 nM和382 nM）。该化合物其MOR部分激动性质展现出镇痛潜力，并可能通通过D3R拮抗作用降低阿片类药物的滥用风险。MOR Agonist-3 亦适用于炎症治痈和神经性疼痛的研究领域。
T61475	Ropivacaine mesylate
	Ropivacaine mesylate 是一种高效的钠通道 (sodium channel) 阻断剂，通过可逆性抑制钠离子内流 (sodium ion influx)，引致神经纤维脉冲传导阻滞。此外，Ropivacaine 还能抑制 K2P(双孔钾通道)TREK-1，其在 COS-7 细胞膜上的 IC50 值为 402.7 μM。
T37374	URB754
	URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fa...
T70077	Fadolmidine HCl
	Fadolmidine, also known as MPV-2426, is a novel and potent alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia. Fadolmidine displayed high affinity and full agonist efficacy at all three human alpha2-adrenoceptor subtypes (A, B and C) in transfected CHO cells with EC50 values (nM) of 0.4, 4.9 and 0.5, respectively. Fadolmidine inhibited also electrically evoked contractions in rat vas deferens demonstrating the activation of rodent presynaptic alpha2D-adrenoceptors with an ...
T73677	SR 142948 dihydrochloride
	SR 142948 dihydrochloride是一种口服活性高、选择性强的非肽类神经降压素受体(NT)拮抗剂，其在h-NTR1-CHO细胞、HT-29细胞和成年大鼠脑中IC50分别为1.19 nM、0.32 nM、3.96 nM。在HT-29细胞中，该化合物能够有效拮抗NT诱导的肌醇单磷酸盐形成，IC50为3.9 nM。此外，SR 142948 dihydrochloride在体内能够阻断NT诱导的体温下降、镇痛和转向行为，且具有良好的血脑屏障通透性，适用于精神疾病研究。
T37391	PSEM 308 hydrochloride
	PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg/kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neu...
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...

化合物

Dexmedetomidine

Cat.No: T2524

Target: Adrenergic Receptor

Cat.No: T6554

Synonym: JZL184

Target: Lipase

Medetomidine hydrochloride

Cat.No: T6579

Synonym: MPV785,Medetomidine HCl,Domitor

Target: Adrenergic Receptor

Methylnaltrexone bromide

Cat.No: T21422

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

Target: Opioid Receptor

Dexmedetomidine hydrochloride

Cat.No: T6466

Synonym: Precedex,(+)-Medetomidine hydrochloride,(S)-Medetomidine hydrochloride,盐酸右美托咪定,Dexmedetomidine HCl

Target: Adrenergic Receptor

Cat.No: T1780

Synonym: SC 69124,帕瑞昔布,Vorth-P,Valus-P

Target: COX

Kyotorphin acetate

Cat.No: T20172L

Target: Endogenous Metabolite, Antibacterial

Cat.No: T50082

Target: Chloride channel

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

Oxeladin citrate

Cat.No: T0056

Target: Others

Levobupivacaine

Cat.No: T1787

Target: Sodium Channel

Propiomazine HCl

Cat.No: T34152L

Synonym: Propiomazine hydrochloride,Largon

Cat.No: T76186

Cat.No: T25675

Synonym: L-Leucinal

Cat.No: T27888

Synonym: LY190388,LY-190388

Cat.No: T70078

Cat.No: T31190

Cat.No: T31541

Synonym: H-L-Tyr-D-Arg-OH

Cat.No: T75919

Cat.No: T80518

Target: Sodium Channel

Cat.No: T32105

Synonym: HSK3486,HSK 3486,HSK-3486

Cat.No: T12970L

Synonym: GW-427,353,GW427353,GW-427353,GW 427,353,GW427,353

Fenobam hydrate

Cat.No: T68959

Cat.No: TP1958

Synonym: PL 017

Dibutyryl-cGMP sodium

Cat.No: T11038

Synonym: Bt2cGMP sodium

Target: Others

Cat.No: T28845

Synonym: SR142948A,SR 142948A,SR-142948A,SR142948A hydrochloride

Cat.No: T37670

β-Endorphin (1-27) (human)

Cat.No: T80515

Target: Opioid Receptor

Hemokinin 1, human TFA

Cat.No: T75840

Cat.No: T81763

Ropivacaine mesylate

Cat.No: T61475

Cat.No: T37374

Fadolmidine HCl

Cat.No: T70077

SR 142948 dihydrochloride

Cat.No: T73677

PSEM 308 hydrochloride

Cat.No: T37391

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat. No.	Product Name	Target	Signaling Pathways
T5691	paulownin 泡桐素	Anti-infection	Microbiology/Virology
	Paulownin 是药用植物的成分，是泡桐木的成分。
T5734	(+)-BORNEOL d-Borneol,(+)-冰片	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	(+)-BORNEOL (d-Borneol) 是一种天然的双环单萜，在中药中用于镇痛和麻醉；增强 GABA 受体活性，EC50 为 248 μM。
T3834	8-Epideoxyloganic acid 8-表去氧马钱酸	ROS; Immunology/Inflammation related	Immunology/Inflammation
	8-Epideoxyloganic acid 是从 Incarvillea delavayi 中分离得到的一种环烯醚萜苷。它具有微弱的缓解疼痛活性。
TN3778	De-4'-O-methylyangambin	Antifection	Microbiology/Virology
	De-4'-O-methylyangambin exhibits antibacterial effects. It also has analgesia activity.

天然产物

Cat.No: T5691

Synonym: 泡桐素

Target: Anti-infection

Cat.No: T5734

Synonym: d-Borneol,(+)-冰片

Target: GABA Receptor

8-Epideoxyloganic acid

Cat.No: T3834

Synonym: 8-表去氧马钱酸

Target: ROS, Immunology/Inflammation related

De-4'-O-methylyangambin

Cat.No: TN3778

Target: Antifection

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