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47

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T14127	Adenosine A1 receptor activator T62	Adenosine Receptor	GPCR/G Protein; Neuroscience
	Adenosine A1 receptor activator T62 是腺苷 A1 受体的变构增强剂，有镇痛作用。
T23283	2-Methoxyidazoxan monohydrochloride RX 821002 hydrochloride	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	L-Albizziin (2-Methoxyidazoxan monohydrochloride) 是高效的 alpha 2r 肾上腺素受体选择性拮抗剂，对 imidazoline 拮抗作用很小或没有。它对 (豚鼠) alpha 2D 肾上腺素受体 (pKd9.7) 的亲和力明显高于 (兔子) alpha 2A 肾上腺素受体 (pKd8.2)。
T22904	L-745870 trihydrochloride L-745870三盐酸盐,L-745,870 trihydrochloride	Dopamine Receptor; Sigma receptor; 5-HT Receptor; Adrenergic Receptor	GPCR/G Protein; Neuroscience
	L-745870 trihydrochloride 是可透过血脑屏障的、选择性的、具有口服活性的多巴胺D4受体拮抗剂，Ki=0.43 nM，而对 D2(Ki 为 960 nM) 和 D3(Ki 为 2300 nM) 受体的亲和力相对较弱，对 5-HT2受体，sigma 位点和 α-肾上腺素受体表现出中等亲和力。
T22905	L748337 L-748,337	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	L748337是一种具有竞争性和高效性的 β3-肾上腺素受体拮抗剂，抑制 β3-、β2- 和 β1-肾上腺素受体发挥作用，激活 MAPK 信号传导，促进 Erk1/2 的磷酸化，抑制CL316243 的保护作用，可用于研究和β3-肾上腺素受体异常引起的疾病。
T22316	Doxazosin UK 33274,多沙唑嗪	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Doxazosin (UK 33274) 是选择性的拮抗突触后的α1肾上腺素受体。
T22052	BU 226 hydrochloride	Imidazoline Receptor	Neuroscience
	BU 226 hydrochloride 对咪唑啉受体具有亲和力，尤其是对 I2 结合位点，Ki 为 1.4 nM。 BU 226 hydrochloride 对 alpha 2-adrenoceptors 显示出低 (microM) 亲和力。
T28895	T-0509 T 0509,T0509	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	T-0509 是一种选择性 beta 1 受体激动剂，可增加犬心室肌的肌力，选择性下调大鼠心脏 β 1-肾上腺素受体。
T10000	(±)-Tazifylline	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	(±)-Tazifylline 是一种选择性的长效组胺 H1 受体拮抗剂。 Tazifylline 对 H2 受体、α- 和 β-肾上腺素能受体、5-羟色胺和毒蕈碱受体亚型的亲和力要低得多。
T13804	OPC-28326	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	OPC-28326 是一种特异性的 α2-肾上腺素能受体拮抗剂，可作为外周血管扩张剂。 OPC-28326 抑制 α2A-、α2B- 和 α2C- 肾上腺素能受体，Ki 分别为 2040、285 和 55nM。
T4978	Sarpogrelate hydrochloride 盐酸沙格雷酯,MCI-9042	5-HT Receptor	GPCR/G Protein; Neuroscience
	Sarpogrelate hydrochloride (MCI-9042) 是一种选择性5-HT2R 拮抗剂，可用于研究与血栓形成有关的血管疾病，对 5-HT2A、5-HT2B 和 5-HT2C 受体的pKi 值分别为 8.52、6.57 和 7.43。
T11277	FG 7142 ZK 39106,LSU-65	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	FG 7142 (LSU-65) 是一种非选择性苯二氮卓类反向激动剂，对含 α1 亚基的 GABAA 受体具有高亲和力，Ki 为 91 nM。它还调节 GABA 诱导的 GABAA 受体上的氯离子通量，表达 α1 亚基，EC50为 137 nM。它可增加酪氨酸羟基化并导致小鼠大脑皮层中 β-肾上腺素受体的上调。
T13376	YS-49	RAAS; Akt; PI3K; Adrenergic Receptor	Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Neuroscience; PI3K/Akt/mTOR signaling
	YS-49 是一种PI3K/Akt(RhoA 的下游靶标) 的激活剂，可减少 3-甲基胆碱处理的细胞中 RhoA/PTEN 的激活。它是异喹啉化合物生物碱，因能激活心脏β-adrenoceptors 而具有强烈的正性肌力作用。它能通过诱导血红素加氧酶来抑制血管紧张素 II 刺激 VSMC 细胞的增殖。
T26784	BFE-61 BFE 61
	BFE-61 is a partial agonist of the beta-adrenoceptors.
T24462	Mezilamine
	Mezilamine is an antagonist of dopamine. It also blocks presynaptic but stimulating postsynaptic alpha-adrenoceptors.
T23878	CH-38083 CH38083
	CH-38083 is a selective and effective alpha-2 adrenoceptors antagonist.
T71447	Perbufylline
	Perbufylline is a bronchodilator. It is N-methylated xanthine derivative. Perbufylline acts as a competitive antagonist at 5-HT2 and alpha1-adrenoceptors, with at least 100-fold less activity at alpha2-adrenoceptors.
T68767	Mezilamine HCl
	Mezilamine HCl is a dopamine antagonist, blocking presynaptic but stimulating postsynaptic alpha-adrenoceptors.
T11763	Ko-3290	Others	Others
	Ko-3290 is a cardioselective antagonist of β-adrenoceptors known for its antilipolytic effects in animals.
T28172	Niguldipine hydrochloride BY-935,Niguldipine HCl,B-85935,B-8509-035,B-859-35
	Niguldipine is a calcium channel antagonist. Niguldipine shows high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors.
T71803	Mabuterol hydrochloride
	Mabuterol hydrochloride is a selective β2 adrenoreceptor agonist. Mabuterol has a specific effect on beta 2-adrenoceptors with no beta 1-stimulation.
T68707	DJ 7141
	DJ 7141 is a unique alpha-2 agonist which shows high affinity to peripheral alpha-2 adrenoceptors but only a mild hypotensive activity.
T11608	Epanolol Visacor,ICI141292	Others	Others
	Epanolol is a potent β-adrenoceptor partial agonist with a greater affinity for β1- than β2-adrenoceptors.
T29906	Alprenolol-nbd Alp-NBD
	Alprenolol-nbd is a fluorescent beta-adrenoceptor probe that binds irreversibly to beta-adrenoceptors and non-receptor binding sites.
T68854	LDT3 HCl
	LDT3 HCl is a potent multi-target antagonists of both alpha1A- and alpha1D-adrenoceptors, and also of 5-HT1A receptors.
T68634	Wy 26392
	Wy 26392 is an alpha 2 adrenoceptors antagonist that increase central sympathetic tone and blood pressure in low doses.
T26783	BFE-55 BFE 55
	BFE-55 is derivative of befunolol (a beta-adrenergic partial agonist). BFE-55 interacts with only the high affinity sites in beta-adrenoceptors
T71335	PF-3774076
	PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors.
T30880	Chir 2279 Chir2279
	Chir 2279 is a N-(substituted)glycine peptoid trimer with high-affinity binding for alpha 1-adrenoceptors. CHIR 2279 antagonized the epinephrine-induced increase in intraurethal pressure (pseudo pA2, 6.86) in dogs.
T68241	Wy 27127
	Wy 27127 is an alpha 2-adrenoceptors antagonist that has estimated potency based on ability to block clonidine-induced inhibition of electrically-evoked contractions of the rat isolated vas deferens.
T17202	Ulimorelin TZP-101	Others	Others
	Ulimorelin is a ghrelin receptor agonist (EC50: 29 nM and a Ki of 16 nM). Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors.
TP1902	G-Protein antagonist peptide
	Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
T62476	Trimazosin
	Trimazosin 是一种口服具有活力的 quinazoline 衍生物，结构与 prazosin 有关。Trimazosin 能够选择性阻断α1肾上腺素受体 (α1-adrenoceptors)，具有降压 (hypotensive) 活性。
T27140	Delequamine HCl RS-15385,RS15385,RS 15385,Delequamine,RS-15385-197
	Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72).
T68825	Doxazosin HCl
	Doxazosin HCl is the salt form of Doxazosin Free Base which acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.
T61729	Terazosin
	Terazosin, a quinazoline derivative, is an orally active and competitive antagonist of α1-adrenoceptors. Its mechanism of action involves relaxing blood vessels and promoting bladder opening. Terazosin exhibits therapeutic potential for treating benign prostatic hyperplasia (BPH) and high blood pressure [1][2][3].
T21492	Medetomidine
	Medetomidine(Domtor)是一种有效的、高选择性的、具有口服活性的α2肾上腺素受体激动剂，对α2和α1肾上腺素受体的 Ki 值分别为1.08 nM 和1750 nM。
TP2086	AdTx1
	Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenylephrine on isolated rabbit prostate
T80477	Muscarinic toxin 3 MT3	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Muscarinic toxin 3 (MT3) 是高效的非竞争性mAChR及adrenoceptors拮抗剂，对M1、M4、α1A、α1B、α1D、α2A、α2B、α2C受体展示出不同程度的选择性，其pIC50值分别为6.71、8.79、8.86、7.57、8.13、8.49、6.5、7.29。该化合物具有显著的肾上腺素受体抑制活性。
T71033	ZD7114 free base
	ZD7114, also known as ICI-D7114, is a selective adrenoceptor agonist of brown fat and thermogenesis. ICI D7114 stimulates thermogenesis at doses that have little effect on beta 1 or beta 2 adrenoceptors. Treatment with ICI D7114 activates BAT and thermogenesis even in species and situations where the intrinsic capacity is low. ICI D7114 has beneficial effects in animal models of obesity and disturbed glucose and lipid homeostasis.
T68183	PPMC
	The alpha-adrenoceptors blocking effect of (N-piperidinomethyl)-2-chromanne was studied in vivo and in vitro in the rat. In the pithed rat, (N-piperidinomethyl)-2-chromanne (1 mg/kg i.v.) antagonized the pressor effects induced by alpha agonists. (N-piperidinomethyl)-2-chromanne competitively antagonized the pressor effects of M7 (alpha 2-agonist) and cirazoline (alpha 1-agonist). (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on presynaptic alpha 2-receptors in...
T60677	Dobutamine
	Dobutamine 是合成儿茶酚胺，可增加心排血量，矫正低灌注。Dobutamine 作用于α1-AR,β1-AR 和β2-AR（α-1、β-1和β-2肾上腺素能受体），是 β1-AR 受体的选择性激动剂，对 α1-AR 和 β2-AR 活性相对较弱。
T75238	YS-49 monohydrate
	YS-49 (单水合物) 作为PI3K/Akt（RhoA的下游靶点）的激活剂，有效降低3-甲基胆碱处理的细胞中RhoA/PTEN的活性。此外，YS-49通过促进血红素加氧酶（HO-1）的表达，抑制血管紧张素II（Ang II）诱导的血管平滑肌细胞（VSMC）增殖。作为一种异喹啉化合物生物碱，YS-49因激活心脏β-adrenoceptors而显示出显著的正性肌力效应。
T61027	Piribedil hydrochloride
	Piribedil hydrochloride 可用于帕金森病，循环系统疾病，癌症等的研究。Piribedil hydrochloride 以0.18 μM 的EC50值抑制 MLL1 甲基转移酶的活性。Piribedil hydrochloride 是口服有效的多巴胺 D2 和多巴胺 D3 激动剂，也是 α2-肾上腺素能受体的拮抗剂。
T60304	(E)-Guanabenz
	(E)-Guanabenz ((E)-Wy-8678) 是一种具有口服活性的中枢α2-肾上腺素受体 (α2-adrenoceptor)激动剂。(E)-Guanabenz 具有抗高血压活性，通过刺激中枢 α2- 肾上腺素受体，并减少交感神经向外周的净流出而起作用。(E)-Guanabenz z 也直接结合并抑制 GADD34，具有神经保护活性。(E)-Guanabenz 可用于研究高血压和帕金森病。
T9451	Bopindolol
	Bopindolol 是一种口服活性的 β-肾上腺素受体 (ARs) 拮抗剂，具有部分激动剂活性。Bopindolol 对 β1- 和 β2-ARs 无选择性，对β3-AR 亚型亲和力低。Bopindolol 是 Pindolol 的前体药物，可迅速代谢为活性水解形式。Bopindolol 可用于原发性和肾血管性高血压的研究。
T40869	Moxonidine hydrochloride BDF5895hydrochloride,盐酸莫索尼定
	Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent. Target: I1-R Moxonidine Hydrochloride is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 +/- 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response...
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 ...

化合物

Adenosine A1 receptor activator T62

Cat.No: T14127

Target: Adenosine Receptor

2-Methoxyidazoxan monohydrochloride

Cat.No: T23283

Synonym: RX 821002 hydrochloride

Target: Adrenergic Receptor

L-745870 trihydrochloride

Cat.No: T22904

Synonym: L-745870三盐酸盐,L-745,870 trihydrochloride

Target: Dopamine Receptor, Sigma receptor, 5-HT Receptor, Adrenergic Receptor

Cat.No: T22905

Synonym: L-748,337

Target: Adrenergic Receptor

Cat.No: T22316

Synonym: UK 33274,多沙唑嗪

Target: Adrenergic Receptor

BU 226 hydrochloride

Cat.No: T22052

Target: Imidazoline Receptor

Cat.No: T28895

Synonym: T 0509,T0509

Target: Adrenergic Receptor

(±)-Tazifylline

Cat.No: T10000

Target: Histamine Receptor

Cat.No: T13804

Target: Adrenergic Receptor

Sarpogrelate hydrochloride

Cat.No: T4978

Synonym: 盐酸沙格雷酯,MCI-9042

Target: 5-HT Receptor

Cat.No: T11277

Synonym: ZK 39106,LSU-65

Target: GABA Receptor

Cat.No: T13376

Target: RAAS, Akt, PI3K, Adrenergic Receptor

Cat.No: T26784

Synonym: BFE 61

Cat.No: T24462

Cat.No: T23878

Synonym: CH38083

Cat.No: T71447

Cat.No: T68767

Cat.No: T11763

Target: Others

Niguldipine hydrochloride

Cat.No: T28172

Synonym: BY-935,Niguldipine HCl,B-85935,B-8509-035,B-859-35

Mabuterol hydrochloride

Cat.No: T71803

Cat.No: T68707

Cat.No: T11608

Synonym: Visacor,ICI141292

Target: Others

Cat.No: T29906

Synonym: Alp-NBD

Cat.No: T68854

Cat.No: T68634

Cat.No: T26783

Synonym: BFE 55

Cat.No: T71335

Cat.No: T30880

Synonym: Chir2279

Cat.No: T68241

Cat.No: T17202

Synonym: TZP-101

Target: Others

G-Protein antagonist peptide

Cat.No: TP1902

Cat.No: T62476

Delequamine HCl

Cat.No: T27140

Synonym: RS-15385,RS15385,RS 15385,Delequamine,RS-15385-197

Cat.No: T68825

Cat.No: T61729

Cat.No: T21492

Cat.No: TP2086

Muscarinic toxin 3

Cat.No: T80477

Synonym: MT3

Target: Adrenergic Receptor

ZD7114 free base

Cat.No: T71033

Cat.No: T68183

Cat.No: T60677

YS-49 monohydrate

Cat.No: T75238

Piribedil hydrochloride

Cat.No: T61027

Cat.No: T60304

Cat.No: T9451

Moxonidine hydrochloride

Cat.No: T40869

Synonym: BDF5895hydrochloride,盐酸莫索尼定

Fadolmidine HCl

Cat.No: T70077

Cat. No.	Product Name	Target	Signaling Pathways
T3232	Higenamine hydrochloride Higenamine HCl,Demethylcoclaurine hydrochloride,盐酸去甲乌头碱,norcoclaurine HCl,(+-)-Demethylcoclaurine hydrochloride,Higenamine Hydrochloride	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Higenamine hydrochloride (norcoclaurine HCl) 是一种 β2-AR 激动剂，是用于心力衰竭相关研究的中药乌头的关键成分，具有抗凋亡活性。
T3S1729	Dihydrolycorine	Others	Others
	Dihydrolycorine 是分离自Lycoris radiate 草药中，是一种真核细胞中蛋白质合成的抑制剂。
T4S0998	Trifolirhizin 红车轴草根甙/三叶豆紫檀苷,三叶豆紫檀苷	TNF; Tyrosinase	Apoptosis; Proteases/Proteasome
	Trifolirhizin 是一种从苦参根中分离出的 pterocarpan 黄酮类化合物。它具有酪氨酸酶高抑制活性，IC50=506 μM。它具有抗炎和抗癌的潜能。
TN4624	Nantenine	Others	Others
	Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca
TN3368	Akuammigine	Opioid Receptor; Adrenergic Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding pA2 values of 4.68. Akuammidine also shows a preference for mu-opioid binding sites with Ki val
T69254	Ajmalicine hydrochloride Raubasine hydrochloride
	Ajmalicine (Raubasine) hydrochloride 是一种有效的抗肾上腺素 (adrenolytic) 剂，优先阻断 α1-肾上腺素受体 (α1-adrenoceptor)。Ajmalicine hydrochloride 是一种可逆性但非竞争性尼古丁受体 (nicotine receptor) 完全抑制剂，其 IC50为 72.3 μM。Ajmalicine hydrochloride 还可用于降压、蛇毒，具有镇静活性。

天然产物

Higenamine hydrochloride

Cat.No: T3232

Synonym: Higenamine HCl,Demethylcoclaurine hydrochloride,盐酸去甲乌头碱,norcoclaurine HCl,(+-)-Demethylcoclaurine hydrochloride,Higenamine Hydrochloride

Target: Adrenergic Receptor

Dihydrolycorine

Cat.No: T3S1729

Target: Others

Cat.No: T4S0998

Synonym: 红车轴草根甙/三叶豆紫檀苷,三叶豆紫檀苷

Target: TNF, Tyrosinase

Cat.No: TN4624

Target: Others

Cat.No: TN3368

Target: Opioid Receptor, Adrenergic Receptor

Ajmalicine hydrochloride

Cat.No: T69254

Synonym: Raubasine hydrochloride

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