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27

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TQ0084	lumateperone Tosylate ITI-007,Lumateperone甲苯磺酸盐	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	lumateperone Tosylate (ITI-007) 是5-HT 2A 受体拮抗剂，Ki 为 0.54 nM，突触前 D2受体的部分激动剂和突触后 D2受体的拮抗剂，Ki 为 32 nM。
T21069	Lumateperone ITI 722,ITI722,ITI-007,卢美哌隆,ITI007	5-HT Receptor	GPCR/G Protein; Neuroscience
	Lumateperone (ITI 722) 是一种 5HT2A 受体拮抗剂和多巴胺受体磷蛋白调节剂 (DPPM)。
T3280	Clodronate disodium tetrahydrate clodronic acid disodium tetrahydrate,Disodium clodronate tetrahydrate,Clastoban,氯屈膦酸二钠(四水合物),Clodronate disodium	IL Receptor; TNF	Apoptosis; Immunology/Inflammation
	Clodronate disodium tetrahydrate (Clastoban) 是一种选择性、高效的，可逆、Cl-竞争性的囊泡核苷酸转运体阻滞剂(IC50:15.6 nM)。是一种双膦酸盐，具有抗骨质疏松、抗炎作用，可用于缓解疼痛的研究。它可抑制神经元释放囊泡 ATP，缓解慢性神经病理性疼痛和炎症性疼痛。
T7386	Bretylium tosylate 溴苄乙胺,托西溴苄铵	Others	Others
	Bretylium tosylate 是交感神经和肾上腺素神经的阻断剂，是血管收缩的神经递质突触前释放的抑制剂。
T21766	ML352
	ML352 是一种突触前胆碱转运体(CHT) 的非竞争性抑制剂，对于表达人 CHT 和小鼠前脑突触体的 HEK293细胞的Ki 值分别为 92 nM 和 166 nM。
T1540	Doxepin hydrochloride Toruan,Doxepin HCl,Aponal,Novoxapin,盐酸多塞平	P450; Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	Doxepin hydrochloride (Aponal) 是一种可口服的三环抗抑郁剂，是选择性组胺受体 H1拮抗剂。它也是 CYP450抑制剂，抑制 CYP450 2C19和 CYP450 1A2。
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。
T0869	Atomoxetine hydrochloride Tomoxetine hydrochloride,(R)-Tomoxetine hydrochloride,盐酸托莫西汀,LY 139603,Atomoxetine HCl,LY 139603 HCl	Dopamine Receptor; 5-HT Receptor; Norepinephrine	GPCR/G Protein; Neuroscience
	Atomoxetine hydrochloride (LY 139603) 是苯氧基-3-丙胺衍生物和选择性非兴奋剂，是去甲肾上腺素再摄取抑制剂，具有认知增强活性。与人 NET，SERT 和 DAT 的放射性配体结合的 Ki 分别为5，77和1451 nM。
T7218	Endomorphin 2 内吗啡肽 2	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Endomorphin 2 是一种高亲和力和选择性的 μ-阿片受体激动剂，对 kappa3 结合位点具有合理的亲和力，Ki 为 20 到 30 nM 之间。
T12118	MSOP	GluR	Neuroscience
	MSOP is a selective antagonist of group III metabotropic glutamate receptor (KD of 51 μM for the L-AP4-sensitive presynaptic mGluR).
T23662	Aganodine Aganodin
	Aganodine is a guanidine that activates presynaptic imidazoline receptors. Aganodine inhibits the presynaptic release of norepinephrine through its agonism at imidazoline receptors.
T10779	CGP 25454A	Others	Others
	CGP 25454A is a novel and selective antagonist of the presynaptic dopamine autoreceptor.
T71439	Opc 4392
	Opc 4392 is an agonist of presynaptic dopamine D(2) receptor.
T68767	Mezilamine HCl
	Mezilamine HCl is a dopamine antagonist, blocking presynaptic but stimulating postsynaptic alpha-adrenoceptors.
T24462	Mezilamine
	Mezilamine is an antagonist of dopamine. It also blocks presynaptic but stimulating postsynaptic alpha-adrenoceptors.
T40541	α-Synuclein (61-75)
	α-Synuclein (61-75) is a peptide fragment derived from the larger protein α-Synuclein. α-Synuclein is predominantly found in presynaptic nerve terminals and is considered to be a biomarker candidate for Parkinson's disease (PD).
T38975	WAY-100135 dihydrochloride
	WAY-100135 dihydrochloride is a potent and selective antagonist of both presynaptic and postsynaptic 5-HT 1A receptors, exhibiting an IC 50 value of 34 nM specifically at the rat hippocampal 5-HT 1A receptor. This compound displays promising antipsychotic effects.
T76187	Dendrotoxin K
	Dendrotoxin K，一种Kv1.1通道阻滞剂，通过时间依赖性地控制突触前尖峰波，从而将谷氨酸释放入CA3神经元中。
T76199	α-Synuclein (61-75) (TFA)
	α-Synuclein(61-75) TFA 是α-Synuclein 的 61-75 片段。α-Synuclein 是一种丰富的神经元蛋白，在突触前神经末梢高度丰富。α-Synuclein 是一种帕金森氏病 (PD) 的生物标志物。
T78062	Dendrotoxin K TFA	Potassium Channel	Membrane transporter/Ion channel
	Dendrotoxin K TFA是一种特异的Kv1.1通道阻滞剂，通过时间依赖性方式调控突触前尖峰波形成，影响到谷氨酸在CA3神经元的释放。
T78456	DASPEI
	DASPEI为具有较大Stokes位移的阳离子苯乙烯基线粒体荧光染料，激发与发射波长分别为550/573 nm，特点是荧光寿命长，灵敏度高。它能对活细胞中线粒体进行有效染色，以及独立于神经元活性，在突触前标记神经末节。
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...
T60492	Lamotrigine hydrate
	Lamotrigine hydrate 是口服有效的抗惊厥剂或抗癫痫剂，通过选择性地阻断电压门控Na+通道，稳定突触前神经元膜并抑制谷氨酸释放。Lamotrigine hydrate 可用于研究癫痫、局灶性癫痫等神经性疾病。
T68190	Carmoxirole (free base)
	Carmoxirole (free base) is a dopamine D2 receptor agonist with limited central activity that modulates sympathetic activation and subsequently reduces pre-load and afterload in animals. It was shown, that carmoxirole induced beneficial effects on hemodynamic and neurohumoral parameters in heart failure. In addition, experimental evidence showed that carmoxirole lowered blood pressure in various models of hypertension mainly or exclusively through inhibition of noradrenaline release from sympathe...
T37608	Riluzole-13C,15N2 Riluzole-13C,15N2
	Riluzole-13C,15N2 is intended for use as an internal standard for the quantification of riluzole by GC- or LC-MS. Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals a...
T20886	Atomoxetine Tomoxetine,HSDB7352,HSDB-7352,HSDB 7352	Norepinephrine	Neuroscience
	Atomoxetine (HSDB 7352) 是一种选择性去甲肾上腺素抑制剂，它可能通过增加外周交感神经元中的去甲肾上腺素浓度而导致血压升高。Atomoxetine 是突触前去 Norepinephrativev 转运体的高度选择性拮抗剂，对其他去甲肾上腺素受体或其他神经递质转运体或受体几乎或没有亲和力，但对5-羟色胺转运体的亲和力较弱。、 Atomoxetine 选择性地抑制去甲肾上腺素的再摄取，可用于治疗患有多动症和慢性抽搐的青少年。
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

lumateperone Tosylate

Cat.No: TQ0084

Synonym: ITI-007,Lumateperone甲苯磺酸盐

Target: Dopamine Receptor, 5-HT Receptor

Cat.No: T21069

Synonym: ITI 722,ITI722,ITI-007,卢美哌隆,ITI007

Target: 5-HT Receptor

Clodronate disodium tetrahydrate

Cat.No: T3280

Synonym: clodronic acid disodium tetrahydrate,Disodium clodronate tetrahydrate,Clastoban,氯屈膦酸二钠(四水合物),Clodronate disodium

Target: IL Receptor, TNF

Bretylium tosylate

Cat.No: T7386

Synonym: 溴苄乙胺,托西溴苄铵

Target: Others

Cat.No: T21766

Doxepin hydrochloride

Cat.No: T1540

Synonym: Toruan,Doxepin HCl,Aponal,Novoxapin,盐酸多塞平

Target: P450, Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor

6-Chloromelatonin

Cat.No: T22530

Target: Melatonin Receptor, Dopamine Receptor

Atomoxetine hydrochloride

Cat.No: T0869

Synonym: Tomoxetine hydrochloride,(R)-Tomoxetine hydrochloride,盐酸托莫西汀,LY 139603,Atomoxetine HCl,LY 139603 HCl

Target: Dopamine Receptor, 5-HT Receptor, Norepinephrine

Cat.No: T7218

Synonym: 内吗啡肽 2

Target: Opioid Receptor

Cat.No: T12118

Target: GluR

Cat.No: T23662

Synonym: Aganodin

Cat.No: T10779

Target: Others

Cat.No: T71439

Cat.No: T68767

Cat.No: T24462

α-Synuclein (61-75)

Cat.No: T40541

WAY-100135 dihydrochloride

Cat.No: T38975

Cat.No: T76187

α-Synuclein (61-75) (TFA)

Cat.No: T76199

Dendrotoxin K TFA

Cat.No: T78062

Target: Potassium Channel

Cat.No: T78456

Cat.No: T68183

Lamotrigine hydrate

Cat.No: T60492

Carmoxirole (free base)

Cat.No: T68190

Riluzole-13C,15N2

Cat.No: T37608

Synonym: Riluzole-13C,15N2

Cat.No: T20886

Synonym: Tomoxetine,HSDB7352,HSDB-7352,HSDB 7352

Target: Norepinephrine

Fadolmidine HCl

Cat.No: T70077

Cat. No.	Product Name	Target	Signaling Pathways
T8118	Bekanamycin Kanamycin B,卡那霉素,卡那霉素 B	Antibacterial; Antibiotic	Microbiology/Virology
	Bekanamycin (Kanamycin B) 是一种提取自 Streptomyces kanamyceticus 的氨基糖苷类抗生素，抑制一系列革兰氏阳性和阴性细菌。
T4S1876	3-Deoxyaconitine	Sodium Channel	Membrane transporter/Ion channel
	3-Deoxyaconitine 是一种二萜类生物碱，对钠离子通道有激活作用。
T8270	Deserpidine 地舍平,Harmonyl	RAAS	Endocrinology/Hormones
	Deserpidine (Harmonyl) 是从 Rauwolfia canescens 的根中分离的生物碱。Deserpidine 与 Reserpine 相关。Deserpidine 是竞争性血管紧张素转化酶抑制剂，可以被用作抗高血压药以及镇定剂。Deserpidine 还减少了肾上腺皮质血管紧张素 II 诱导的醛固酮分泌。

天然产物

Cat.No: T8118

Synonym: Kanamycin B,卡那霉素,卡那霉素 B

Target: Antibacterial, Antibiotic

3-Deoxyaconitine

Cat.No: T4S1876

Target: Sodium Channel

Cat.No: T8270

Synonym: 地舍平,Harmonyl

Target: RAAS

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