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63

抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21793	CGP 35348	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	CGP 35348 是 GABAB 受体的选择性拮抗剂 (EC50 = 34 μM)。 CGP 35348 可用于研究白化新生小鼠脑损伤后的神经肌肉协调和空间学习。
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。
T1247	Clonidine hydrochloride Clonidine HCl,Catapres,盐酸可乐定	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Clonidine hydrochloride (Catapres) 是一种α2-adrenoceptor 激动剂，是一种抗高血压药。
T2150	Guanfacine hydrochloride 盐酸胍法辛,Tenex,Intuniv,Guanfacine	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Guanfacine hydrochloride (Intuniv) 是一种 α2A 肾上腺素受体激动剂，Kd=31 nM，具有抗高血压作用。
T7045	Clonidine Nexiclon,Catapres,Kapvay,可乐定	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Clonidine (Kapvay) 是 alpha2 肾上腺素能激动剂。
T0201	Meptazinol hydrochloride Meptazinol HCl,盐酸美普他酚	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Meptazinol hydrochloride (Meptazinol HCl) 是一种独特的中枢opioid 类镇痛剂，用作具有镇痛特性的麻醉拮抗剂。
T0015	Mephenesin Cresoxydiol,甲酚甘油醚,Memphenesin,Mephedan,Decontractyl	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	Mephenesin (Cresoxydiol) 是 NMDA 受体拮抗剂，也是中枢性肌松弛剂。
T0470	Nefopam hydrochloride 盐酸奈福泮,Fenazoxine hydrochloride,Nefopam HCl	Wnt/beta-catenin; Sodium Channel	Cytoskeletal Signaling; Membrane transporter/Ion channel; Stem Cells
	Nefopam hydrochloride (Nefopam HCl) 作用于体外和体内间充质细胞β-连环蛋白水平，是一种中枢性但非阿片类缓解中度和重度疼痛。
T2571	Benactyzine hydrochloride Neuroleptone,胃复康,盐酸贝那替嗪,Tranquilline,Amitakon	AChR; AChE	Neuroscience
	Benactyzine hydrochloride (Neuroleptone) 是丁酰胆碱酯酶抑制剂，其Ki=0.010 mM。
T60107	N-0500 HCl (-)-Propyl-9-hydroxynaphthoxazine Hydrochloride,那高利特盐酸盐	Dopamine Receptor	GPCR/G Protein; Neuroscience
	N-0500 HCl ((-)-Propyl-9-hydroxynaphthoxazine Hydrochloride) 是一种非常有效的中枢作用 DA 受体激动剂。N-0500 HCl 是[3H]DP_x005f_x0002_5,6-ADTN 特异性结合的有效置换剂，IC50为3nM。
T0922	Zoxazolamine NSC 24995,Contrazole,氯苯恶唑胺,苯并恶唑胺	Others	Others
	Zoxazolamine (NSC-24995) 是排尿酸和肌肉松弛剂，被广泛用于药物测试，可作为啮齿动物细胞色素 P-450 活性变化的方便指标。
T16757	Risdiplam RO7034067,RG7916	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Risdiplam (RO7034067) 是一种中枢和外周分布的 SMN2 前 mRNA 剪接修饰剂，可增加运动神经元存活 (SMN) 蛋白水平。
T7579	1-BCP Piperonylic acid piperidide	GluR; iGluR	Membrane transporter/Ion channel; Neuroscience
	1-BCP (Piperonylic acid piperidide) 是一种调节 AMPA 受体门控电流的中枢活性药物，可增强记忆。
T1650	Chlorzoxazone Paraflex,Chlorzoxazon,氯唑沙宗	P450; Potassium Channel	Membrane transporter/Ion channel; Metabolism
	Chlorzoxazone (Chlorzoxazon) 是作用于中枢的肌肉松弛剂, 可用于肌肉痉挛的研究。
TQ0082	Aticaprant LY-2456302,CERC-501	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Aticaprant (LY-2456302) 是一种有效的中枢渗透性 kappa-阿片受体拮抗剂，Ki 值为 0.807 nM。
T22689	CP94253 hydrochloride CP 94253 hydrochloride	Others; 5-HT Receptor	GPCR/G Protein; Neuroscience; Others
	CP94253 hydrochloride (CP 94253 hydrochloride) 是一种有效的、特异性的和中枢活性的 5-HT1B 受体激动剂，Ki 为 2 nM。5-HT1A、5-HT1D、5-HT1C 和 5-HT2 的 Ki 分别为 89、49、860 和 1600 nM 。
T1509	Cyclobenzaprine hydrochloride 盐酸环苯扎林,Cyclobenzaprine HCl,MK130 hydrochloride	5-HT Receptor	GPCR/G Protein; Neuroscience
	Cyclobenzaprine hydrochloride (MK130 hydrochloride) 是一种具有抗抑郁活性的中枢作用肌肉松弛剂，可减少肌肉痉挛。
T9857L	Vasopressin acetate Vasopressin acetate (11000-17-2 Free base)	Endogenous Metabolite	Metabolism
	Vasopressin acetate 是一种环状九肽，在下丘脑中枢合成。 Vasopressin acetate 作为一种神经递质，通过与特定的 G 蛋白偶联受体结合发挥其作用。
T21439	Tacrine 他克林,CS 12602,Tacrinum,Tetrahydroaminocrine	AChR	Neuroscience
	Tacrine (CS 12602) 一种间接胆碱能激动剂和中枢作用的抗胆碱酯酶。它被批准用于治疗阿尔茨海默病。
T20062	Thiamine disulfide 二硫化硫胺,TDS,Daiomin,Algoneurina	HIV Protease; Endogenous Metabolite	Metabolism; Microbiology/Virology; Proteases/Proteasome
	Thiamine disulfide (Algoneurina) 是一种存在于食物中的维生素，可作为膳食补充剂和药物生产。它还充当许多中枢代谢酶的辅助因子。
T1336	Benztropine mesylate Benzotropine mesylate,苯扎托品,Benzatropine mesylate,Benztropine methanesulfonate,甲磺酸苯扎托品	Dopamine Receptor; AChR; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Benztropine mesylate (Benztropine methanesulfonate) 是一种可口服的中枢性抗胆碱能剂，用于帕金森氏病的研究。它是抗组胺剂，抑制多巴胺的吸收。它也是人 D2多巴胺受体的变构拮抗剂，具有抗癌症干细胞的作用。
T1409	Methocarbamol Lumirelax,美索巴莫,Metocarbamol,AHR 85,Robaxin	Sodium Channel; Carbonic Anhydrase	Membrane transporter/Ion channel; Metabolism
	Methocarbamol (AHR 85) 是口服有效的中枢肌肉松弛剂，可阻断肌肉Nav1.4通道，阻断作用具有可逆性。Methocarbamol 具有用于肌肉痉挛和疼痛综合症研究的潜力。
T68087	Inaperisone	Others	Others
	Inaperisone 是一种新型的中枢作用的肌肉松弛剂，对排尿反射有抑制作用。Inaperisone 可能通过间接作用于脑干的GABAB 受体来抑制排尿反射。
T3724	Rolapitant hydrochloride Rolapitant HCl,罗拉匹坦盐酸盐	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Rolapitant (SCH619734) hydrochloride 是一种高效选择性和具有口服活性的神经激肽 1 (NK1) 受体拮抗剂，Ki 值为 0.66 nM。Rolapitant hydrochloride (Rolapitant HCl) 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的中枢介导的止吐活性。
T0511	Tolperisone hydrochloride 盐酸托哌酮,Muscalm,Midocalm,托哌酮盐酸盐,Tolperisone HCl	Sodium Channel	Membrane transporter/Ion channel
	Tolperisone hydrochloride (Muscalm) 是中枢作用肌肉松弛剂，可用于研究神经疾病引起的病理性横纹肌硬化(锥体束损伤、脊髓病、多发性硬化症、脑脊髓炎)、痉挛性麻痹及其他肌肉张力障碍相关的脑病。
T34281	Relamorelin BIM28131,RM 131,BIM-28131,BIM-28163,BIM 28163,BIM28163,BIM 28131	GHSR	GPCR/G Protein
	Relamorelin (RM-131)是一种具有选择性和有效性的生长素释放肽/生长激素促分泌素受体 (GHSR) 激动剂，是一种有效的生长素释放肽模拟物，对 GHS-1a 受体具有很高的亲和力。Relamorelin 是一种具有中枢渗透性的五肽，可增加生长激素水平，加速胃排空，具有研究恶病质的潜力。
T3716	Rolapitant 罗拉吡坦,SCH619734,罗拉匹坦	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂，Ki 值为0.66 nM。
T28778	Silperisone HCl RGH5002,SILA336,RGH-5002,Silperisone hydrochloride,SILA-336
	Silperisone HCl (RGH-5002) 阻断细胞中的钠和钙通道，使肌肉细胞的兴奋度和收缩度降低，降低外周张力，充当肌肉松弛剂和外周血管扩张剂。 Silperisone HCl 可用于治疗脊髓损伤引起的复发性疼痛性肌阵挛、脑血管病引起的异常高肌张力、肌张力症状、锥体紧张综合征、多发性硬化症肌痉挛和脊髓炎。Silperisone 是钠通道蛋白2型α通道阻滞剂。Silperisone 是一种类似于tolperisone 的有机硅化合物，具有中枢作用的肌肉松弛剂特性。
T70503	Exp 631
	Exp 631 is a centrally-acting non-opioid analgesic; exhibits serotonin and norepinephrine reuptake inhibiting activities.
T69422	Flupirtine HCl
	Flupirtine HCl is the salt form of Flupirtine, also known as W-2964, an aminopyridine that functions as a centrally acting non-opioid analgesic. It first became available in Europe in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor. Like nefopam, it is unique among analgesics in that it is a non-opioid, non-NSAID, non-steroidal centrally acting analgesic. Flupirtine is a selective neuronal potassium channel opener that also has NMDA re...
T11722	JNJ-37822681 dihydrochloride	Dopamine Receptor	GPCR/G Protein; Neuroscience
	JNJ-37822681 dihydrochloride 是特异性的、有中枢活性的，可快速解离的多巴胺 D2受体拮抗剂，与多巴胺 D2L 受体结合的亲和力适中 (Ki=158 nM)。JNJ-37822681 dihydrochloride 在精神分裂症和躁郁症领域有研究价值。
T34668	Snf 8814 Snf-8814,Snf8814
	Snf 8814 is an analog of centrally selective cholecystokinin.
T29950L	Ambenoxan hydrochloride Ambenoxan HCl
	Ambenoxan hydrochloride is a centrally acting skeletal muscle relaxant.
T19690	SB 224289 SB224289,SB-224289
	SB 224289 is a selective antagonist of 5-HT1B receptor with pKi of 8.2. It is a centrally active following oral administration in vivo. SB 224289 displays 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand
T2571L	Benactyzine
	Benactyzine is a centrally acting muscarinic antagonist.
T29950	Ambenoxan Ambenoxanum
	Ambenoxan is a centrally acting muscle relaxant.
T26902	Bremazocine
	Bremazocineis a potent opiate kappa-agonist and centrally acting analgesic.
T15591	Ipenoxazone NC-1200,MLV-6976,伊培沙宗	Others	Others
	Ipenoxazone is an effective and centrally acting muscle relaxant.
T28970	Tiamenidine Hoe-440
	Tiamenidine is an antagonist of centrally-acting alpha1 adrenergic receptor.
T26924	Butamirate
	Butamirate is a cough suppressant, it works by acting centrally through the receptors in the brainstem.
T27685	JNJ-42314415 JNJ 42314415,JNJ42314415
	JNJ-42314415 is a potent, specific, and centrally active inhibitor of PDE10A.
T69169	Tiamenidine hydrochloride
	Tiamenidine hydrochloride is a centrally-acting alpha1 adrenergic receptor antagonist.
T14361	Axomadol 阿索马多,EN3324	Others	Others
	Axomadol (EN3324) is a centrally active analgesic compound. It has opioid agonistic properties and inhibitory effects on the reuptake of monoamines.
T21376	Chlorphenesin Carbamate Kolpicortin-sine,Rinlaxer,Chlorphensin carbamate,Maolate,氯苯氨酸甘油酯,laChlorphenesin Carbamate
	Chlorphenesin Carbamate is a centrally acting muscle relaxant used to treat muscle pain and spasms and also an antifungal agent.
T21077	Tolperisone free base Mydeton,Atmosgen free base,Mideton,Menopatol,Besnoline free base,Mydocalm
	Tolperisone free base, a centrally acting muscle relaxant, has been used for the symptomatic treatment of spasticity and muscle spasm.
T23781	Benzatropine Akitan,Benztropine,NK 02,Cogentinol,Cogentine
	Benzatropine is a centrally active muscarinic antagonist. It also inhibits the uptake of dopamine. It has been used in the symptomatic treatment of Parkinson's Disease.
T11070L	DO34	Others	Others
	DO34 is a highly potent and centrally active inhibitor of diacylglycerol lipase (IC50: 6 nM for DAGLα conversion of SAG to 2-AG).
T31105	CS 722 CS-722,CS722
	CS 722 is a centrally acting muscle relaxant. CS-722 exerts its muscle relaxant action by affecting both the supraspinal structure and the spinal cord.
T22435	Tacrine hydrochloride 四氢氨基吖啶,盐酸他克林,Tacrine HCl	Others	Others
	Tacrine is a indirect cholinergic agonist and centrally acting anticholinesterase. Tacrine hydrochloride hydrate is an inhibitor of acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
T68779	CE-178,253
	CE-178,253 is a selective centrally-acting CB1 receptor antagonist.

化合物

Cat.No: T21793

Target: GABA Receptor

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

Clonidine hydrochloride

Cat.No: T1247

Synonym: Clonidine HCl,Catapres,盐酸可乐定

Target: Adrenergic Receptor

Guanfacine hydrochloride

Cat.No: T2150

Synonym: 盐酸胍法辛,Tenex,Intuniv,Guanfacine

Target: Adrenergic Receptor

Cat.No: T7045

Synonym: Nexiclon,Catapres,Kapvay,可乐定

Target: Adrenergic Receptor

Meptazinol hydrochloride

Cat.No: T0201

Synonym: Meptazinol HCl,盐酸美普他酚

Target: Opioid Receptor

Cat.No: T0015

Synonym: Cresoxydiol,甲酚甘油醚,Memphenesin,Mephedan,Decontractyl

Target: NMDAR, iGluR

Nefopam hydrochloride

Cat.No: T0470

Synonym: 盐酸奈福泮,Fenazoxine hydrochloride,Nefopam HCl

Target: Wnt/beta-catenin, Sodium Channel

Benactyzine hydrochloride

Cat.No: T2571

Synonym: Neuroleptone,胃复康,盐酸贝那替嗪,Tranquilline,Amitakon

Target: AChR, AChE

Cat.No: T60107

Synonym: (-)-Propyl-9-hydroxynaphthoxazine Hydrochloride,那高利特盐酸盐

Target: Dopamine Receptor

Cat.No: T0922

Synonym: NSC 24995,Contrazole,氯苯恶唑胺,苯并恶唑胺

Target: Others

Cat.No: T16757

Synonym: RO7034067,RG7916

Target: DNA/RNA Synthesis

Cat.No: T7579

Synonym: Piperonylic acid piperidide

Target: GluR, iGluR

Cat.No: T1650

Synonym: Paraflex,Chlorzoxazon,氯唑沙宗

Target: P450, Potassium Channel

Cat.No: TQ0082

Synonym: LY-2456302,CERC-501

Target: Opioid Receptor

CP94253 hydrochloride

Cat.No: T22689

Synonym: CP 94253 hydrochloride

Target: Others, 5-HT Receptor

Cyclobenzaprine hydrochloride

Cat.No: T1509

Synonym: 盐酸环苯扎林,Cyclobenzaprine HCl,MK130 hydrochloride

Target: 5-HT Receptor

Vasopressin acetate

Cat.No: T9857L

Synonym: Vasopressin acetate (11000-17-2 Free base)

Target: Endogenous Metabolite

Cat.No: T21439

Synonym: 他克林,CS 12602,Tacrinum,Tetrahydroaminocrine

Target: AChR

Thiamine disulfide

Cat.No: T20062

Synonym: 二硫化硫胺,TDS,Daiomin,Algoneurina

Target: HIV Protease, Endogenous Metabolite

Benztropine mesylate

Cat.No: T1336

Synonym: Benzotropine mesylate,苯扎托品,Benzatropine mesylate,Benztropine methanesulfonate,甲磺酸苯扎托品

Target: Dopamine Receptor, AChR, Histamine Receptor

Cat.No: T1409

Synonym: Lumirelax,美索巴莫,Metocarbamol,AHR 85,Robaxin

Target: Sodium Channel, Carbonic Anhydrase

Cat.No: T68087

Target: Others

Rolapitant hydrochloride

Cat.No: T3724

Synonym: Rolapitant HCl,罗拉匹坦盐酸盐

Target: Neurokinin receptor

Tolperisone hydrochloride

Cat.No: T0511

Synonym: 盐酸托哌酮,Muscalm,Midocalm,托哌酮盐酸盐,Tolperisone HCl

Target: Sodium Channel

Cat.No: T34281

Synonym: BIM28131,RM 131,BIM-28131,BIM-28163,BIM 28163,BIM28163,BIM 28131

Target: GHSR

Cat.No: T3716

Synonym: 罗拉吡坦,SCH619734,罗拉匹坦

Target: Neurokinin receptor

Silperisone HCl

Cat.No: T28778

Synonym: RGH5002,SILA336,RGH-5002,Silperisone hydrochloride,SILA-336

Cat.No: T70503

Cat.No: T69422

JNJ-37822681 dihydrochloride

Cat.No: T11722

Target: Dopamine Receptor

Cat.No: T34668

Synonym: Snf-8814,Snf8814

Ambenoxan hydrochloride

Cat.No: T29950L

Synonym: Ambenoxan HCl

Cat.No: T19690

Synonym: SB224289,SB-224289

Cat.No: T2571L

Cat.No: T29950

Synonym: Ambenoxanum

Cat.No: T26902

Cat.No: T15591

Synonym: NC-1200,MLV-6976,伊培沙宗

Target: Others

Cat.No: T28970

Synonym: Hoe-440

Cat.No: T26924

Cat.No: T27685

Synonym: JNJ 42314415,JNJ42314415

Tiamenidine hydrochloride

Cat.No: T69169

Cat.No: T14361

Synonym: 阿索马多,EN3324

Target: Others

Chlorphenesin Carbamate

Cat.No: T21376

Synonym: Kolpicortin-sine,Rinlaxer,Chlorphensin carbamate,Maolate,氯苯氨酸甘油酯,laChlorphenesin Carbamate

Tolperisone free base

Cat.No: T21077

Synonym: Mydeton,Atmosgen free base,Mideton,Menopatol,Besnoline free base,Mydocalm

Cat.No: T23781

Synonym: Akitan,Benztropine,NK 02,Cogentinol,Cogentine

Cat.No: T11070L

Target: Others

Cat.No: T31105

Synonym: CS-722,CS722

Tacrine hydrochloride

Cat.No: T22435

Synonym: 四氢氨基吖啶,盐酸他克林,Tacrine HCl

Target: Others

Cat.No: T68779

Cat. No.	Product Name	Target	Signaling Pathways
T0086	Galanthamine hydrobromide Galantamine hydrobromide,Galanthamine HBr,氢溴酸加兰他敏	AChR; AChE	Neuroscience
	Galanthamine hydrobromide (Galantamine hydrobromide) 是一种长效的中枢活性 AChE 抑制剂，IC50为 410 nM。它是神经元烟碱型 ACh 受体的变构增强剂，IC50值为 0.35 µM，可用于阿尔茨海默症的研究。
T0965	Histamine Ergamine,组胺	5-HT Receptor; Endogenous Metabolite; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	Histamine (Ergamine) 是通过组胺的酶促脱羧衍生的胺。它是一种强大的胃分泌兴奋剂、支气管平滑肌的收缩剂、血管扩张剂以及中枢作用的神经递质。
T6534	Histamine dihydrochloride 组胺二盐酸盐,peremin,Ceplene,Histamine 2HCl	Endogenous Metabolite; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	Histamine dihydrochloride (Ceplene) 是 Histamine 的二盐酸形式。Histamine 是一种有机氮化合物，是一种强效的胃分泌兴奋剂，支气管平滑肌收缩剂，血管舒张剂，也是一种中枢作用的神经递质。

天然产物

Galanthamine hydrobromide

Cat.No: T0086

Synonym: Galantamine hydrobromide,Galanthamine HBr,氢溴酸加兰他敏

Target: AChR, AChE

Cat.No: T0965

Synonym: Ergamine,组胺

Target: 5-HT Receptor, Endogenous Metabolite, Histamine Receptor

Histamine dihydrochloride

Cat.No: T6534

Synonym: 组胺二盐酸盐,peremin,Ceplene,Histamine 2HCl

Target: Endogenous Metabolite, Histamine Receptor

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