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37

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3278	Piribedil EU-4200,Trivastan,ET-495,Trivastal	Dopamine Receptor; Histone Methyltransferase; Adrenergic Receptor	Chromatin/Epigenetic; GPCR/G Protein; Neuroscience
	Piribedil (Trivastan) 是多巴胺 D2受体激动剂，对 hα1A-肾上腺素受体也显示出拮抗作用。
T21935L	AMN082 free base AMN082	GluR	Neuroscience
	AMN082 free base 是 mGluR7选择性激动剂，口服有活性，能够透过血脑屏障，可通过跨膜区的变构位点直接激活受体信号。在表达 mGluR7 的转染哺乳动物细胞上，它能够有效抑制 cAMP 积累并刺激 GTPγS 结合。它能够选择性针对 mGluR 的其他亚型及选择性离子型谷氨酸受体。具有抗抑郁活性。
T6140	SB-334867 free base SB334867A free base,SB-334867,SB 334867,SB334867	OX Receptor	GPCR/G Protein; Neuroscience
	SB-334867 free base (SB334867A free base) 是一种选择性 orexin-1(OX1) 受体拮抗剂，对 OX2有选择性，pKb 为7.4，对 5-HT2B、5-HT2C 的选择性是 100 倍，pKi 值分别为 5.4 和 5.3。它减少乙醇消耗，还抑制吗啡诱导的体内运动活动敏感性的获得。
T21935	AMN082 AMN 082 dihydrochloride	GluR	Neuroscience
	AMN082 (AMN 082 dihydrochloride) 是可口服，可透过血脑屏障的选择性mGluR7激动剂，通过跨膜区的变构位点直接激活受体信号，具有抗抑郁作用。
T35033	Vamicamide FK 176,FK-176,FK176	AChE	Neuroscience
	Vamicamide (FK 176)是一种新型抗胆碱能化合物。Vamicamide 在 32 mg/kg （p.o.）或更高时增加小鼠的自发运动活动，并在 100 mg/kg 时抑制小鼠强直性惊厥。
T35033L	(S)-Vamicamide (S)-Vamicamide (Iso-132373-81-0)	AChE	Neuroscience
	(S)-Vamicamide 是一种新型抗抗胆碱能化合物。Vamicamide 在 32 mg/kg 或更高（p.o.）时增加小鼠的自发运动活动，并在 100 mg/kg 时抑制小鼠强直性惊厥。
T21792	CGP 3466B maleate 马来酸CGP3466B,Omigapil (Maleate),Omigapil maleate	Apoptosis	Apoptosis
	CGP 3466B maleate (Omigapil maleate) 是一种口服有效的 GAPDH 亚硝基化抑制剂，可消除 Aβ1-42 诱导的小鼠 tau 乙酰化，记忆障碍和运动功能障碍，Omigapil maleate 具有研究阿尔茨海默症的潜力。Omigapil maleate (CGP3446B maleate) 是一种有效的凋亡 (apoptosis) 抑制剂。Omigapil maleate 可用于研究先天性肌营养不良 (CMD)。
TP1940L1	Ac-RYYRIK-NH2 acetate	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Ac-RYYRIK-NH2 acetate 是 nociceptin/orphanin FQ(noc/OFQ) 受体的激动剂，影响自发运动活动。它是转染在 CHO 细胞中的 ORL1 的部分激动剂，可拮抗大鼠脑膜和切片中 noc/OFQ 对 [35S]-GTPgammaS 与 G 蛋白结合的刺激。
T3685	SR9009 Stenabolic,REV-ERB Agonist II	Autophagy	Autophagy
	SR9009 (Stenabolic) 是一种REV-ERBα/β激动剂，可增加由 REV-ERBα/ERBβ 调节的基因的组成性抑制，IC50分别为 670 nM 和 800 nM。
T37190	L-Allylglycine	Dehydrogenase; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	L-Allylglycine 是 GABA 合成酶（谷氨酸脱羧酶）的有效抑制剂。
T32440	L 363572 L363-572,L-363572,L-363-572,L363572,L 363-572
	L 363572, a hexapeptide analog of MK 678, does not effect locomotor acitivity in rats.
TP1983	Neuropeptide S (human)
	Potent endogenous neuropeptide S receptor agonist (EC50 = 9.4 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.
T75951	Neuropeptide S(Rat) TFA
	Neuropeptide S(Rat) TFA, a robust endogenous agonist for the neuropeptide S receptor (NSPR) with an EC50 of 3.2 nM, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.
T81659	NocII TFA
	NocII TFA 是孤儿神经肽，能刺激小鼠运动。
T28313	PD 117302 PD-117302,PD117302
	PD 117302 is a nonpeptide opioid compound. It is a selective kappa-opioid agonist. PD 117302 causes naloxone-reversible locomotor impairment and diuresis. It is an Anti-Arrhythmia Agent, an Anticonvulsants, a Cardiovascular Agent, and a Central Nervous Sy
TP1981	Neuropeptide S(Mouse) Neuropeptide S (Mouse)
	Potent endogenous neuropeptide S receptor (NPSR) agonist (EC50 = 3 nM). Induces mobilization of intracellular Ca2+. Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.
TP1982	Neuropeptide S(Rat) Neuropeptide S (Rat)
	Potent endogenous neuropeptide S receptor (NSPR) agonist (EC50 = 3.2 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.
TP1980	Neuromedin S(rat) Neuromedin S (rat)
	Potent, endogenous neuromedin U receptor agonist (EC50 values are 65 and 91 pM at NMU1 and NMU2 respectively). Induces phase shifts in the circadian rhythm of locomotor activity following i.c.v. administration. Potent endogenous anorexigenic peptide.
TP1940	Ac-RYYRIK-NH2
	High affinity ligand for the NOP site (Ki = 1.5 nM). Antagonizes nociceptin-stimulated GTP binding in rat brain and the chronotropic effect of nociceptin on rat cardiomyocytes. However, displays potent agonist properties in vivo, inhibiting locomotor acti
T82587	Delta (Phospho) Sleep Inducing Peptide DSIP-P
	Delta (Phospho) Sleep Inducing Peptide (DSIP-P) 是促进睡眠效应持久的多肽，能诱导大鼠昼夜运动行为的改变。
T75915	CTOP TFA
	CTOP TFA为高效、高选择性μ-阿片受体(μ-opioid receptor)拮抗剂。其能拮抗吗啡引发的急性镇痛效果及运动能力增强，同时升高伏隔核外多巴胺水平，并呈剂量依赖性增强运动能力。
T60270	(R)-Preclamol
	(R)-Preclamol 是一种具有自身受体和突触后受体刺激特性的多巴胺 (DA) 激动剂。(R)-Preclamol 以低剂量抑制小鼠和大鼠的运动活动。
T29230	ZK-95962
	ZK-95962 is an agonist gamma-aminobutyric acid (GABA) receptor. ZK-95962 had selective effects on releasing exploratory locomotor activity suppressed by footshock (punished crossings). ZK-95962 had weak effects on the measures of anxiolytic activity. The
T38172	RO 5263397 hydrochloride
	Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 \|Galley et al (2015) Discovery ...
T75950	Neuropeptide S(Mouse) TFA
	Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.
T71327	Paraxanthine-d6
	Paraxanthine-d6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine is an adenosine A1 and A2 receptor antagonist. In vivo, paraxanthine increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity, as well as inhibits motor depression induced by the adenosine A1 agoni...
TP1986	[Arg14,Lys15]Nociceptin
	Highly potent and selective NOP receptor agonist (EC50 = 1 nM). Displays > 875-fold selectivity over opioid receptors (IC50 values are 0.32, 280, > 10000 and 1500 for NOP, μ, δ and κ receptors respectively). Longer lasting and 30-fold more potent than noc
T80900	Unasnemab MT-3921,rH116A3
	Unasnemab (MT-3921)，一种人源化IgG1单克隆抗体，与排斥引导分子A (RGMa) 结合，用以改善运动功能及促进神经再生，适用于脊髓损伤研究。
T29206	ZCZ011 ZCZ 011,ZCZ-011
	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
T35785	N-Oleoyl Leucine
	N-Oleoyl leucine is an N-acyl amide generated by PM20D1 that uncouples mitochondrial respiration independent of uncoupling protein 1 (UCP1) in vitro. N-Oleoyl leucine (25 mg/kg, i.p.) decreases body weight and food intake, preferentially decreasing fat mass in a diet-induced obesity mouse model. It improves glucose homeostasis in a fasting glucose tolerance test and increases VO2 while slightly decreasing overall locomotor activity.
T38221	N,N-Dipropyldopamine (hydrobromide)
	N,N-Dipropyldopamine is a dopamine receptor agonist.1,2,3 It decreases dihydrophenylalanine (DOPA) levels in the limbic forebrain and striatum of reserpinized rats (ED50s = 25 and 20 μmol/kg, respectively), as well as reduces homovanillic acid levels in rat striatum when administered at a dose of 80 μmol/kg.1 N,N-Dipropyldopamine (0.5-16 mg/kg) reduces spontaneous locomotor activity in mice, an effect that can be reversed by the antipsychotic spiroperidol.2,3
T23099	O-2050	Others	Others
	O-2050 是一种高亲和力的大麻素CB1受体拮抗剂，Ki 为 2.5 nM。O-2050 抑制大麻素 CB2受体，Ki 为 0.2 nM。O-2050 减少了小鼠的食物摄入量，并且引起小鼠运动。
T83166	Adipokinetic hormone (Gryllus bimaculatus) Grybi-AKH
	Adipokinetic hormone Gryllus bimaculatus (Grybi-AKH) 是调节昆虫能量平衡的脂肪动力激素，主要功能是动员脂肪体内的脂质和碳水化合物。此外，Grybi-AKH也能增强双斑蟋蟀的运动活性，并在人体体重调节、体重减轻及糖原贮积障碍缓解的研究中具有应用潜力。
TP1989	NEP(1-40) Nogo-66 (1-40)
	Peptide fragment corresponding to residues 1 - 40 of Nogo-66, the domain of the myelin protein Nogo that inhibits axonal outgrowth. Acts as a competitive antagonist at the Nogo-66 receptor (NgR); blocks Nogo-66- and CNS myelin-induced inhibition of axonal
T36499	CuATSM
	The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility ...
T71000	RO-5328673
	RO-5328673 is a dual NK2/NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of g...
T37094	(S)-UFR2709 hydrochloride (S)-UFR2709 hydrochloride
	(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction[1][2]. Brain nicotinic acetylcholine receptors (nAChRs) is a heterogeneous family of pentameric acetylcholine-gated cation channels, whi...

化合物

Cat.No: T3278

Synonym: EU-4200,Trivastan,ET-495,Trivastal

Target: Dopamine Receptor, Histone Methyltransferase, Adrenergic Receptor

AMN082 free base

Cat.No: T21935L

Synonym: AMN082

Target: GluR

SB-334867 free base

Cat.No: T6140

Synonym: SB334867A free base,SB-334867,SB 334867,SB334867

Target: OX Receptor

Cat.No: T21935

Synonym: AMN 082 dihydrochloride

Target: GluR

Cat.No: T35033

Synonym: FK 176,FK-176,FK176

Target: AChE

Cat.No: T35033L

Synonym: (S)-Vamicamide (Iso-132373-81-0)

Target: AChE

CGP 3466B maleate

Cat.No: T21792

Synonym: 马来酸CGP3466B,Omigapil (Maleate),Omigapil maleate

Target: Apoptosis

Ac-RYYRIK-NH2 acetate

Cat.No: TP1940L1

Target: Opioid Receptor

Cat.No: T3685

Synonym: Stenabolic,REV-ERB Agonist II

Target: Autophagy

Cat.No: T37190

Target: Dehydrogenase, GABA Receptor

Cat.No: T32440

Synonym: L363-572,L-363572,L-363-572,L363572,L 363-572

Neuropeptide S (human)

Cat.No: TP1983

Neuropeptide S(Rat) TFA

Cat.No: T75951

Cat.No: T81659

Cat.No: T28313

Synonym: PD-117302,PD117302

Neuropeptide S(Mouse)

Cat.No: TP1981

Synonym: Neuropeptide S (Mouse)

Neuropeptide S(Rat)

Cat.No: TP1982

Synonym: Neuropeptide S (Rat)

Neuromedin S(rat)

Cat.No: TP1980

Synonym: Neuromedin S (rat)

Cat.No: TP1940

Delta (Phospho) Sleep Inducing Peptide

Cat.No: T82587

Synonym: DSIP-P

Cat.No: T75915

Cat.No: T60270

Cat.No: T29230

RO 5263397 hydrochloride

Cat.No: T38172

Neuropeptide S(Mouse) TFA

Cat.No: T75950

Paraxanthine-d6

Cat.No: T71327

[Arg14,Lys15]Nociceptin

Cat.No: TP1986

Cat.No: T80900

Synonym: MT-3921,rH116A3

Cat.No: T29206

Synonym: ZCZ 011,ZCZ-011

N-Oleoyl Leucine

Cat.No: T35785

N,N-Dipropyldopamine (hydrobromide)

Cat.No: T38221

Cat.No: T23099

Target: Others

Adipokinetic hormone (Gryllus bimaculatus)

Cat.No: T83166

Synonym: Grybi-AKH

Cat.No: TP1989

Synonym: Nogo-66 (1-40)

Cat.No: T36499

Cat.No: T71000

(S)-UFR2709 hydrochloride

Cat.No: T37094

Synonym: (S)-UFR2709 hydrochloride

Cat. No.	Product Name	Target	Signaling Pathways
TMS1461	Qingyangshengenin B 青阳参甙元B,青阳参苷元B,Otophylloside B	Beta Amyloid	Neuroscience
	Qingyangshengenin B (Otophylloside B) 是一种分离自 Qingyangshen 的 C-21 甾体苷。它能够在 mRNA 水平上抑制 Aβ 的表达来减少 Aβ 的沉积，对 Aβ 的毒性有保护作用。它具有抗癫痫作用。
TN4722	Otophylloside F	Others	Others
	Otophylloside F can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.

天然产物

Qingyangshengenin B

Cat.No: TMS1461

Synonym: 青阳参甙元B,青阳参苷元B,Otophylloside B

Target: Beta Amyloid

Otophylloside F

Cat.No: TN4722

Target: Others

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