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Search Results for " anxiolytic-like "

28

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21995	XAP044	GluR	Neuroscience
	XAP044 是高效的选择性mGlu7拮抗剂。代谢型谷氨酸受体亚型 7 是哺乳动物 CNS 中神经传递的重要突触前调节剂。它在啮齿动物行为测试中表现出较好的大脑暴露、广谱抗应激、抗抑郁以及抗焦虑作用。
T19916	TRIM 1-(2-Trifluoromethylphenyl)imidazole,1-(2-三氟甲基苯基)咪唑	NOS	Immunology/Inflammation
	TRIM (1-(2-Trifluoromethylphenyl)imidazole) 是一氧化氮合酶抑制剂。它在体外能够抑制小鼠小脑 nNOS (IC50:28.2 µM)，以及大鼠肺 iNOS (IC50:27.0 µM)。它拥有抗焦虑以及抗抑郁的能力。
T23007	MM 77 dihydrochloride MM 77二盐酸盐	5-HT Receptor	GPCR/G Protein; Neuroscience
	MM 77 dihydrochloride 是一种有效的 5-HT1A 受体突触后拮抗剂，具有抗焦虑样活性。
T16421	p-MPPI hydrochloride	5-HT Receptor	GPCR/G Protein; Neuroscience
	p-MPPI hydrochloride 是一种选择性的，具有高亲和力的5-HT1A 受体拮抗剂，能穿过血脑屏障，具有抗抑郁和抗焦虑样作用。
T23509	VU 0285683	GluR	Neuroscience
	VU 0285683 是 mGluR5 的特异性负变构调节剂，对 MPEP 结合位点具有高亲和力。 VU 0285683 表现出抗焦虑样活性。
TP1889	MCL0020 MCL 0020	Melanocortin Receptor	GPCR/G Protein; Neuroscience
	MCL0020 是一种有效的选择性黑素皮质素MC4受体拮抗剂，IC50为 11.63 nM。它剂量依赖性减轻束缚应激诱发的厌食症，在体内表现出抗焦虑样活性。
T16408	Osanetant SR142801	Others	Others
	Osanetant produces anxiolytic- and antidepressant-like effects. Osanetant is a selective NK3 receptor antagonist. It is researched for schizophrenia.
T27744	KRM-II-81 KRM-II81,KRM-II 81
	KRM-II-81 is a γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand. KRM-II-81 exhibits improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.
T40205	Posovolone Co 134444
	Posovolone (Co 134444), an orally active neuroactive steroid with sedative-hypnotic properties, exhibits anticonvulsant and anxiolytic-like activities, alongside ataxic effects.
T13192	TPA-023B	Others	Others
	TPA-023B is an orally active and high-affinity agonist of the GABAA receptor α2/α3 subtype (Kis: 0.73 nM/2 nM) partial and an antagonist α1 subtype (Ki: 1.8 nM), has non-sedating anxiolytic-like properties.
T70292	DDPM-2571 HCl
	DDPM-2571 is a highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties. DDPM-2571 was quickly distributed into the brain and was highly effective in the prevention of chemically-induced seizures (pentylenetetrazole and pilocarpine models) and 6-Hz convulsions. It demonstrated significant anxiolytic-like and antidepressant-like properties. DDPM-2571 had antinociceptive properties, both in the hot plate...
T70021	Oleanolic acid acrylate
	Oleanolic acid acrylate (OAA) is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A and a derivative of oleanolic acid. It is also a selective inhibitor of MAO-A with anti-depressant-like and anxiolytic activities.
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.
T61506	NBI-31772 hydrate
	NBI-31772 hydrate is a powerful inhibitor of the interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). It acts as a nonpeptide ligand, effectively releasing bioactive IGF-I from the IGF-I/IGFBP-3 complex (Ki values for all six human subtypes range from 1-24 nM). This compound demonstrates significant anxiolytic and antidepressant-like effects [1] [2] [3].
T21625	BW 723C86 hydrochloride
	BW-723C86 是一种有效的选择性5-HT2B 受体激动剂，可导致大鼠食欲过盛和梳理毛发减少。BW-723C86 表现出类抗焦虑作用。
T74413	(S)-Osanetant
	(S)-Osanetant 是 Osanetant 的S 对映体。Osanetant (SR142801) 是一种选择性的NK3受体拮抗剂。Osanetant 有抗焦虑和抗抑郁的作用，并被研究用于精神分裂症。
TP1557	Urocortin II, human TFA
	Human urocortin (hUcn) II is a new member of the corticotropin-releasing-factor (CRF) family. It selectively binds to the CRF2 receptor. Human urocortin II exhibits mild motor-suppressive effects and delayed anxiolytic-like effects，suggesting a time-depen
T37823	M 084 hydrochloride
	TRPC4/5 channel blocker (IC50 values are 3.7-10.3 and 8.2 μM, respectively). Also weakly blocks TRPC3 channels. Exhibits rapid antidepressant and anxiolytic effects in vivo. Zhu et al (2015) Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels. Br.J.Pharmacol. 172 3495 PMID:25816897 \|Yang et al (2015) Acute treatment with a novel TRPC4/C5 channel inhibitor produces antidepressant and anxiolytic-like effects in mice. PLoS One 10 e0136...
T73568	MTEP
	MTEP，一种非竞争性且高选择性的mGluR5拮抗剂，具有显著的抗抑郁和抗焦虑效果，亦被用于帕金森疾病的研究。
T80423	Phoenixin-20 PNX-20	Epigenetic Reader Domain	Chromatin/Epigenetic
	Phoenixin-20（PNX-20）为脊椎动物内具激素样生物活性肽，能激活下丘脑-垂体-性腺轴，调控哺乳类生殖过程。该肽通过CREB-PGC-1α途径增进神经元线粒体生物发生。
T78094	Eglumegad hydrochloride LY354740 hydrochloride,Eglumetad hydrochloride
	Eglumegad (LY354740) hydrochloride是一种高效且选择性的group II (mGlu2/3) receptor激动剂，其对人mGlu2和mGlu3受体的IC50值分别是5和24 nM。该化合物能够保护神经元不受NMDA毒性影响，并表现出抗焦虑及抗精神病样作用。
TP2136	(d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin
	Selective vasopressin V1A receptor antagonist. Inhibits vasopressin and oxytocin-induced increases in intracellular calcium concentrations in vitro (IC50 values are 5 and 30 nM respectively). Exhibits potent and prolonged antivasopressor activity and indu
T80424	Phoenixin-20 TFA PNX-20 TFA	Epigenetic Reader Domain	Chromatin/Epigenetic
	Phoenixin-20 (TFA) (PNX-20 (TFA)) 是一种在脊椎动物中发挥激素作用的生物活性肽，能够激活下丘脑-垂体-性腺轴，从而调控哺乳类动物的生殖机能。此外，该肽通过CREB-PGC-1α途径，增强神经元的线粒体生物生成。
T75812	MMK1 TFA
	MMK1 TFA 是一种有效的选择性人甲酰肽受体样 1 (FPRL-1/FPR2) 激动剂，对 FPRL-1 和 FPR1 的 EC50值分别为 <2 nM 和 >10000 nM。MMK1 TFA 是一种有效的趋化剂和钙动员 (calcium-mobilizing) 激动剂。MMK1 TFA 可有效激活吞噬性白细胞，并可增强人单核细胞对百日咳毒素敏感的促炎细胞因子 IL-1b 和IL-6的产生。MMK1 TFA 发挥抗焦虑样活性。
T75832	Cyclotraxin B TFA
	Cyclotraxin B TFA 是一种环肽，是一种高效且选择性的 TrkB 抑制剂，且不会改变 BDNF 的结合。Cyclotraxin B TFA 非竞争性地抑制 BDNF 诱导的 TrkB 活性，IC50值为 0.30 nM。Cyclotraxin B TFA 可以穿越血脑屏障，并具有止痛和抗焦虑的行为作用。
T37114	SB 242084 dihydrochloride
	SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9....
T37194	5α-Androst-16-en-3α-ol
	5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.1,2It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50= 0.4 μM).25α-Androst-16-en-3α-ol (0.1-1 μM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α1β2γ2and α2β2γ2subunit-containing GABAAreceptors.In vivo, 5α-androst-16-en-3α-ol (5-10 mg/kg) decreases immobility time in the forced s...
T38145	Eltoprazine
	Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of no...

化合物

Cat.No: T21995

Target: GluR

Cat.No: T19916

Synonym: 1-(2-Trifluoromethylphenyl)imidazole,1-(2-三氟甲基苯基)咪唑

Target: NOS

MM 77 dihydrochloride

Cat.No: T23007

Synonym: MM 77二盐酸盐

Target: 5-HT Receptor

p-MPPI hydrochloride

Cat.No: T16421

Target: 5-HT Receptor

Cat.No: T23509

Target: GluR

Cat.No: TP1889

Synonym: MCL 0020

Target: Melanocortin Receptor

Cat.No: T16408

Synonym: SR142801

Target: Others

Cat.No: T27744

Synonym: KRM-II81,KRM-II 81

Cat.No: T40205

Synonym: Co 134444

Cat.No: T13192

Target: Others

Cat.No: T70292

Oleanolic acid acrylate

Cat.No: T70021

Fenobam hydrate

Cat.No: T68959

NBI-31772 hydrate

Cat.No: T61506

BW 723C86 hydrochloride

Cat.No: T21625

Cat.No: T74413

Urocortin II, human TFA

Cat.No: TP1557

M 084 hydrochloride

Cat.No: T37823

Cat.No: T73568

Cat.No: T80423

Synonym: PNX-20

Target: Epigenetic Reader Domain

Eglumegad hydrochloride

Cat.No: T78094

Synonym: LY354740 hydrochloride,Eglumetad hydrochloride

(d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin

Cat.No: TP2136

Phoenixin-20 TFA

Cat.No: T80424

Synonym: PNX-20 TFA

Target: Epigenetic Reader Domain

Cat.No: T75812

Cyclotraxin B TFA

Cat.No: T75832

SB 242084 dihydrochloride

Cat.No: T37114

5α-Androst-16-en-3α-ol

Cat.No: T37194

Cat.No: T38145

Cat. No.	Product Name	Target	Signaling Pathways
T3886	Rosavin Rosavidin,络塞维	P450	Metabolism
	Rosavin (Rosavidin) 是从R. rosea 中获得的，在小鼠模型中表现出抗抑郁、适应原性和抗焦虑样作用。
T8014	Epoxylinalool 氧化芳樟醇,2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran	Others	Others
	Epoxylinalool (2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran) 是一种天然存在的单萜醇，广泛用于香水和调味品的生产。
T6S2227	Spinosin 斯皮诺素,Flavoayamenin	Others	Others
	Spinosin (Flavoayamenin) 是一种具有神经保护作用的 C-糖苷类黄酮，从 Zizyphus jujube 种子分离得到，能够激活 Nrf2/HO-1 通路，并抑制 Aβ1-42的产生和聚合。
TCS0102	Pulegone 胡薄荷酮,(+)-Pulegone,蒲勒酮，胡薄荷酮，长叶薄荷酮	Calcium Channel; Endogenous Metabolite; TRP/TRPV Channel	Membrane transporter/Ion channel; Metabolism
	Pulegone ((+)-Pulegone) 是 Calamintha nepeta (L.) Savi 的精油的主要化学成分，也是禽类驱虫剂之一。它在禽类物种中驱避作用的分子靶点是伤害感受性 TRP 锚蛋 1。它刺激鸡感觉神经元中的 TRPM8 和 TRPA1 通道，并在高浓度下抑制前者但不抑制后者。
TN4322	Isopulegol	ATPase; Potassium Channel; GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GABAA receptors and to antioxidant properties.Isopulegol presents significant gastroprotective effects in both ethanol- and indomethacin-induced ulcer models, which appear to be mediated, at least in part, by endogenous prostaglandins, K(ATP) channel opening, and antioxidant proper...

天然产物

Cat.No: T3886

Synonym: Rosavidin,络塞维

Target: P450

Cat.No: T8014

Synonym: 氧化芳樟醇,2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran

Target: Others

Cat.No: T6S2227

Synonym: 斯皮诺素,Flavoayamenin

Target: Others

Cat.No: TCS0102

Synonym: 胡薄荷酮,(+)-Pulegone,蒲勒酮，胡薄荷酮，长叶薄荷酮

Target: Calcium Channel, Endogenous Metabolite, TRP/TRPV Channel

Cat.No: TN4322

Target: ATPase, Potassium Channel, GABA Receptor

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