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25

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1463	Ramelteon 雷美替胺,TAK-375	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	Ramelteon (TAK-375) 是强效高选择性和可口服的 MT1/MT2激动剂，Ki 值分别为 14 和 112 pM，有用于失眠症的研究潜力。
T3722	MK-1064 Urokinase inhibitor 1,MK 1064	OX Receptor	GPCR/G Protein; Neuroscience
	MK-1064 (Urokinase inhibitor 1) 是一种选择性食欲素 2 (2-SORA)受体拮抗剂，可用于失眠患者的研究。
T12877L	Seltorexant JNJ-42847922	OX Receptor	GPCR/G Protein; Neuroscience
	Seltorexant (JNJ-42847922) 是一种可口服，高亲和性以及选择性的 orexin-2 受体(OX2R)拮抗剂，对人和大鼠中的 OX2R 的pKi 值分别为 8.0 和 8.1。它穿过血脑屏障，迅速占据大鼠大脑中的 OX2R 结合位点。
T14983	Clomethiazole Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE	P450; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Clomethiazole (Distraneurin) 是口服GABAA 激动剂，可抑制人肝微粒体中的细胞色素 P450 异构体，CYP2A6 和 CYP2E1。它有抗惊厥作用，具有治疗惊厥性癫痫持续状态的潜力。
T41143	pCPA methyl ester hydrochloride 4-氯-DL-苯基丙氨酸甲酯盐酸盐,4-Chloro-DL-phenylalanine methyl ester hydrochloride	5-HT Receptor; Hydroxylase	GPCR/G Protein; Metabolism; Neuroscience
	pCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) 是色氨酸羟化酶抑制剂和5-HT 合成的抑制剂。 pCPA methyl ester hydrochloride 可穿过血脑屏障并降低 5-HT 中枢可用性。
T67782	Daridorexant hydrochloride Nemorexant hydrochloride,Quviviq	OX Receptor	GPCR/G Protein; Neuroscience
	Daridorexant hydrochloride (Nemorexant hydrochloride) 是一种新型的双Orexin 受体拮抗剂。Daridorexant hydrochloride 可用于失眠研究。
T5500	DORA-22	OX Receptor	GPCR/G Protein; Neuroscience
	DORA-22 是一种双食欲素受体拮抗剂，可改善轻度压力引起的失眠，对记忆的影响很小。
T30188L	Atagabalin HCl PD-0200390 HCl,Atagabalin HCl(223445-75-8 Free base）	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Atagabalin HCl 是一种新型电压依赖性钙通道（VDCC）α2δ亚基（1 和 2）配体，会影响慢波睡眠,可用于治疗失眠。
T37979	N-Desmethyl Pimavanserin AC-279	5-HT Receptor	GPCR/G Protein; Neuroscience
	N-Desmethyl Pimavanserin (AC-279) 是 Pimavanserin (一种 5-HT2A 受体反向激动剂）的活性代谢物，可用于治疗失眠等睡眠障碍。
T1619	Trazodone hydrochloride KB-831,盐酸曲唑酮,Trazodone HCl,AF-1161	5-HT Receptor; Adrenergic Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Trazodone hydrochloride (Trazodone HCl) 是5 羟色胺受体拮抗剂和重吸收抑制剂，用作抗抑郁药，可治疗失眠和焦虑。
T22530	6-Chloromelatonin	Melatonin Receptor; Dopamine Receptor	GPCR/G Protein; Neuroscience
	6-Chloromelatonin 是一种有效的褪黑素受体 (melatonin receptor) 激动剂，是一种5-甲氧基吲哚化合物，可竞争兔视网膜中相同的突触前褪黑激素受体位点，可抑制[3H]多巴胺的钙依赖性释放具有比褪黑素更高的代谢稳定性。6-Chloromelatonin 竞争 [3H] 褪黑素与 MT2 受体结合 (pKi=9.77)，可能用于研究与抑郁症相关的失眠和睡眠障碍。
T68469	NBI-75043
	NBI-75043 is a histamine H1 receptor antagonist, for potential use in the treatment of insomnia.
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.
T29008	Triclofos Sodium SCH-10159,SCH 10159,SCH10159
	Triclofos Sodium is used to treat insomnia and used for sedation.
T38139	Orexin receptor antagonist 2
	Orexin Receptor Antagonist 2 (compound 30), characterized by its potent antagonistic activity with pKis of 7.69 and 9.78, holds promise for insomnia research[1].
T69715	ORN-0829 hydrate
	ORN-0829 hydrate is a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia.
T72954	Fazamorexant YZJ-1139
	Fazamorexant (YZJ-1139) 为高效食欲素受体拮抗剂，主要应用于失眠研究之中。
T61088	Propiomazine
	Propiomazine is an orally active antihistamine agent that possesses sedative properties. It finds utility in insomnia research [1] [2].
T26061	Reposal WT-161,Reposamal,Reposal novo,WT161,WT 161
	Reposal is a barbiturate derivative invented in the 1960s in Denmark. It has hypnotic, sedative, and anticonvulsant properties, and was used primarily for the therapy of insomnia.
T30188	Atagabalin PD 0200390,PD-0200390,PD0200390
	Atagabalin, also known as PD 0200390, is a gabamimetic agent under development for the treatment for insomnia. Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2). It was discontinued following unsatisfactory t
T69063	Orvepitant
	Orvepitant is a potent and selective NK1 antagonist, which may be potentially useful for patients with major depressive disorder (MDD), anxiety and insomnia.
T39004	Vornorexant ORN-0829,TS-142
	Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC 50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia treatment research.
T32833	Lobeline, (+)- (+)-Lobeline
	Lobeline, (+)- is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has been proposed for a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, a
T69420	Vestipitant
	Vestipitant, also known as GW597599, is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.
T69419	Vestipitant mesylate
	Vestipitant mesylate is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

化合物

Cat.No: T1463

Synonym: 雷美替胺,TAK-375

Target: Melatonin Receptor, MT Receptor

Cat.No: T3722

Synonym: Urokinase inhibitor 1,MK 1064

Target: OX Receptor

Cat.No: T12877L

Synonym: JNJ-42847922

Target: OX Receptor

Cat.No: T14983

Synonym: Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE

Target: P450, GABA Receptor

pCPA methyl ester hydrochloride

Cat.No: T41143

Synonym: 4-氯-DL-苯基丙氨酸甲酯盐酸盐,4-Chloro-DL-phenylalanine methyl ester hydrochloride

Target: 5-HT Receptor, Hydroxylase

Daridorexant hydrochloride

Cat.No: T67782

Synonym: Nemorexant hydrochloride,Quviviq

Target: OX Receptor

Cat.No: T5500

Target: OX Receptor

Cat.No: T30188L

Synonym: PD-0200390 HCl,Atagabalin HCl(223445-75-8 Free base）

Target: Calcium Channel

N-Desmethyl Pimavanserin

Cat.No: T37979

Synonym: AC-279

Target: 5-HT Receptor

Trazodone hydrochloride

Cat.No: T1619

Synonym: KB-831,盐酸曲唑酮,Trazodone HCl,AF-1161

Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor

6-Chloromelatonin

Cat.No: T22530

Target: Melatonin Receptor, Dopamine Receptor

Cat.No: T68469

Cat.No: T32105

Synonym: HSK3486,HSK 3486,HSK-3486

Triclofos Sodium

Cat.No: T29008

Synonym: SCH-10159,SCH 10159,SCH10159

Orexin receptor antagonist 2

Cat.No: T38139

ORN-0829 hydrate

Cat.No: T69715

Cat.No: T72954

Synonym: YZJ-1139

Cat.No: T61088

Cat.No: T26061

Synonym: WT-161,Reposamal,Reposal novo,WT161,WT 161

Cat.No: T30188

Synonym: PD 0200390,PD-0200390,PD0200390

Cat.No: T69063

Cat.No: T39004

Synonym: ORN-0829,TS-142

Cat.No: T32833

Synonym: (+)-Lobeline

Cat.No: T69420

Vestipitant mesylate

Cat.No: T69419

Cat. No.	Product Name	Target	Signaling Pathways
TL0002	Liquiritin apioside	Others	Others
	Liquiritin apioside 是一种从甘草中获得的黄酮，具有镇咳活性。
T22357	Lobeline sulfate 硫酸山梗菜碱,Lobelin sulphate	Others	Others
	Lobelin sulphate is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in insomnia, and smoking cessation, peripheral vascular disorders, respiratory disor

天然产物

Liquiritin apioside

Cat.No: TL0002

Target: Others

Lobeline sulfate

Cat.No: T22357

Synonym: 硫酸山梗菜碱,Lobelin sulphate

Target: Others

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