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67

抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T6164 Ciproxifan

FUB-359,环丙基[4-[3-(1H-咪唑-4-基)丙氧基]苯基]甲酮马来酸盐

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Ciproxifan (FUB-359) 是一种高效且特异性的组胺 H3 受体拮抗剂,IC50值为 9.2 nM,可用于研究衰老性疾病和阿尔兹海默症。
T41247 Thioperamide maleate

MR-12842 maleate,硫丙咪胺马来酸

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Thioperamide maleate (MR-12842 maleate) 是一种有效且选择性的 H3 受体拮抗剂 (Ki = 4.3 nM),可抑制 [3H]histamine 的合成 (Ki = 31 nM)。
T22864 Immethridine dihydrobromide

Others Others
Immethridine dihydrobromide is a histamine H3 receptor agonist.
T67828 Enerisant

Enerisant 是一种组胺H3受体拮抗剂/逆激动剂。体外研究表明,Enerisant 是一种有效的、高选择性的、竞争性的组胺H3受体拮抗剂,其选择性比其他组胺受体亚型高3000倍以上。
T27678 JNJ-39220675

JNJ39220675

JNJ-39220675, a selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats.
T10499 H3 receptor-MO-1

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
H3 receptor-MO-1 是一种有效的组胺 H3 受体 (histamine H3 receptor) 调节剂,可用于研究神经分裂和认知障碍。
T7413 JNJ-5207852

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
JNJ-5207852 是一种新型的非咪唑组胺 H3 受体拮抗剂,其对大鼠和人 H3 受体的 pKi 值分别为 8.9 和9.24。
TQ0066 GSK189254A

GSK189254

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
GSK189254A (GSK189254) 是一种有效的特异性组胺 H3 受体拮抗剂,对人类和大鼠H3的pKi 值分别为9.59到9.90和8.51到9.17之间。
T60636 Pitolisant

Pitolisant 是一种有效的选择性的非咪唑类反相激动剂,作用于重组人组胺H3受体反相激动剂,Ki 值为 0.16 nM。
T79500L KSK94 FA

KSK94 FA(2566716-07-0 Free base)

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
KSK94 FA 是一种高效的组胺 H3 受体拮抗剂,抑制 H3 受体,可用于研究神经性疼痛和肥胖症。
T7176 Pitolisant hydrochloride

1-[3-[3-(4-氯丙基)丙氧基]丙基]-哌啶盐酸盐,BF 2649,Ciproxidine

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Pitolisant hydrochloride (Ciproxidine) 是一种有效的、选择性的组胺 H3 受体反向激动剂,Ki 为0.16 nM。
T8822 JNJ-5207852 dihydrochloride

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
JNJ-5207852 dihydrochloride 是一种新型的非咪唑组胺 H3 受体拮抗剂,对大鼠和人类 H3受体的 pKi 值分别为 8.9 和 9.24。
T77593 KSK67

Sigma receptor GPCR/G Protein
KSK67 是一种具有选择性的 sigma-2 和 组胺 H3 受体双重拮抗剂,对 H3 受体、sigma-1、sigma-2 受体有抑制作用, Ki 值分别为 3.2, 1531, 101 nM。KSK67 可用于研究伤害性疼痛和神经性疼痛。
T79499 KSK68

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
KSK68 是一种高效的 sigma-1 和 组胺 H3 受体双重拮抗剂,具有潜在的镇痛活性,对 H3 受体、sigma-1、sigma-2 受体有很高的亲和力。KSK68 可用于研究与疼痛相关的疾病。
T14087 ABT-239

TRP/TRPV Channel Membrane transporter/Ion channel
ABT-239是一种新型、高效、非咪唑类H3R 拮抗剂,也是一种TRPV1拮抗剂。
T70489 Enerisant HCl

P450; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
Enerisant HCl是一种新型强效选择性组胺H3受体拮抗剂,是P-gp的底物,由细胞色素P450(CYP)和转运蛋白介导。
T12054L MK-0249 FA

MK-0249 FA(862309-06-6 Free base)

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
MK-0249 FA 是一种具有口服活性、选择性和高效性的组胺 H3 反向激动剂,可用于研究成人注意力缺陷、多动症神经分裂和认知障碍。
T0246 Betahistine dihydrochloride

PT-9,Betahistine 2HCl,盐酸倍他司汀

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Betahistine dihydrochloride (Betahistine 2HCl) 是可口服的组胺 H1 受体激动剂和 H3 受体的拮抗剂,可用作血管扩张剂,用于类风湿性关节炎的研究。
T32191 Irdabisant

CEP-26401,CEP 26401,CEP26401

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Irdabisant (CEP-26401) 是选择性、口服活性和血脑屏障渗透性的组胺 H3 受体 (histamine H3 receptor, H3R) 拮抗剂/逆激动剂。Irdabisant 显示人 H3R 和大鼠 H3R 的 Ki 分别为 2.0 nM 和 7.2 nM。Irdabisant 抑制 hERG 电流的活性相对较低 (IC50= 13.8 μM)。在大鼠社会认知模型中,Irdabisant 具有认知增强和唤醒作用。Irdabisant 可用于研究精神分裂症或认知障碍。
T8514 LML134

LML-134

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
LML134 (LML-134) 是一种可口服的高选择性组胺 H3 受体反向激动剂,有用于过度睡眠障碍的潜力,对 hH3R 的 cAMP 和 bdg 的Kis 分别为 0.3 和 12 nM。
T4195 Betahistine

PT 9 base,倍他司汀,Vasomotal,Serc base

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Betahistine (Vasomotal) 是可口服的组胺 H1 受体激动剂和 H3 受体的拮抗剂,可用作血管扩张剂,用于类风湿性关节炎的研究。
T1232 Mepyramine maleate

马来酸吡纳明,Pyrilamine maleate,吡拉明马来酸盐

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Mepyramine maleate (Pyrilamine maleate) 是一种组胺 H1 拮抗剂,对 H1、H2 和 H3 受体的 Kd 值分别为 0.8、5200 和大于 3000 nM,对 H1 受体的 pKd 值为 9.4。它是感冒药的常见成分,具有温和的催眠特性和局部麻醉作用,可用于胃肠外和局部过敏。
T14970 Cipralisant

GT-2331

Others Others
Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorde
T12054 MK-0249

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
MK-0249 is a potent antagonist of histamine H3 receptor (human H3, Ki : 1.7 nM).
T70112 GT-2227

GT-2227 is a histamine H3 receptor antagonist.
T70111 GT-2394

GT-2394 is a histamine H3 receptor agonist.
T23456 Thioperamide

Others Others
histamine H3 and H4 antagonist/inverse agonist
T71270 ZEL-H16

ZEL-H16 is an agonist of the histamine H3 receptor.
T27473 GSK334429

GSK-334429,GSK 334429

GSK334429 is an antagonist of histamine H3 receptor.
T22878 JNJ 10181457 dihydrochloride

Others Others
JNJ 10181457 dihydrochloride is a Histamine H3 receptor antagonist.
T23038 Nα-Methylhistamine dihydrochloride

Others Others
Nα-Methylhistamine dihydrochloride is a histamine H3 receptor agonist.
T23841 Burimamide

Burimamide is an antagonist of histamine. It appears to block both H2 and H3 histamine receptors.
T28184 NNC-38-1049

NNC381049,NNC 38-1049,NNC38-1049,NNC 381049,NNC-381049

NNC-38-1049 is a novel selective antagonist of histamine H3.
T23190 Proxyfan oxalate

Others Others
histamine H3 receptor ligand
T29043 UCL-1972

UCL 1972

UCL-1972, a Histamine H3 Receptor Antagonist, used to treat cognitive disorders.
T69756 GT-2331

GT-2331 is a histamine H3 receptor antagonist.
T12416 PF-03654746 Tosylate

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
PF-03654746 Tosylate is selective antagonist of histamine H3 receptor with high brain penetration.
T24698 (R)-(-)-α-Methylhistamine dihydrochloride

HISTAMINE DIHYDROCHLORIDE R(-)-A-METHYL

R(-)-alpha-Methylhistamine 2HCl is an effective and selective agonist of the H3 histamine receptor.
T69737 SCH-79687

SCH-79687 is a histamine antagonist selective for the H3 subtype. This H3 antagonist may play a role in allergic rhinitis.
T22863 Immepip dihydrobromide

Others Others
Immepip dihydrobromide is a histamine H3 receptor agonist.
T23519 VUF 5681 dihydrobromide

Others Others
histamine H3 receptor silent antagonist
T26643 Aplysamine-1

Aplysamine

Aplysamine-1 is an antagonist of histamine H3 receptor.
T10911 H3 receptor antagonist 1

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.
T12630 (R)-(-)-α-Methylhistamine dihydrobromide

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective agonist of H3 histamine receptor( Kd of 50.3 nM).
T27022 Cipralisant maleate

GT-2331,Cipralisant maleate. trade name Perceptin,GT 2331,GT2331

Cipralisant maleate is a potent, selective Histamine H3 receptor antagonist.
T15565 Imetit dihydrobromide

VUF 8325 dihydrobromide,SKF 91105 dihydrobromide

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Imetit dihydrobromide is a high affinity and effective agonist of histamine H3 and H4 receptors (Ki: 0.3 and 2.7 nM). Imetit mimics the histamine effect in triggering a shape change in eosinophils (EC50: 25 nM).
T71605 APD-916 dicitrate

APD-916 dicitrate is a potent and selective inverse agonist of the histamine H3 receptor.
T19628 GSK 189254 HCl

GSK-189254A,GSK 189254A,GSK 189254 hydrochloride,GSK189254A

GSK 189254A is a histamine H3 receptor antagonist for the treatment of narcolepsy. Histamine H3 receptor antagonists have been shown to increase the release of neurotransmitters in the brain and to enhance cognition in vivo. The compound may also be usefu
T22866 Impentamine dihydrobromide

Others Others
Impentamine dihydrobromide is a histamine H3 receptor antagonist.
T15590 Iodophenpropit dihydrobromide

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Iodophenpropit dihydrobromide is an effective and selective antagonist of the histamine H3 receptor. The binding of [125I]Iodophenpropit is readily reversible, selective, and of high affinity (KD: 0.32 nM).

化合物

Ciproxifan
Cat.No: T6164
Synonym: FUB-359,环丙基[4-[3-(1H-咪唑-4-基)丙氧基]苯基]甲酮马来酸盐
Target: Histamine Receptor
Thioperamide maleate
Cat.No: T41247
Synonym: MR-12842 maleate,硫丙咪胺马来酸
Target: Histamine Receptor
Immethridine dihydrobromide
Cat.No: T22864
Synonym:
Target: Others
Enerisant
Cat.No: T67828
Synonym:
Target:
JNJ-39220675
Cat.No: T27678
Synonym: JNJ39220675
Target:
H3 receptor-MO-1
Cat.No: T10499
Synonym:
Target: Histamine Receptor
JNJ-5207852
Cat.No: T7413
Synonym:
Target: Histamine Receptor
GSK189254A
Cat.No: TQ0066
Synonym: GSK189254
Target: Histamine Receptor
Pitolisant
Cat.No: T60636
Synonym:
Target:
KSK94 FA
Cat.No: T79500L
Synonym: KSK94 FA(2566716-07-0 Free base)
Target: Histamine Receptor
Pitolisant hydrochloride
Cat.No: T7176
Synonym: 1-[3-[3-(4-氯丙基)丙氧基]丙基]-哌啶盐酸盐,BF 2649,Ciproxidine
Target: Histamine Receptor
JNJ-5207852 dihydrochloride
Cat.No: T8822
Synonym:
Target: Histamine Receptor
KSK67
Cat.No: T77593
Synonym:
Target: Sigma receptor
KSK68
Cat.No: T79499
Synonym:
Target: Histamine Receptor
ABT-239
Cat.No: T14087
Synonym:
Target: TRP/TRPV Channel
Enerisant HCl
Cat.No: T70489
Synonym:
Target: P450, Histamine Receptor
MK-0249 FA
Cat.No: T12054L
Synonym: MK-0249 FA(862309-06-6 Free base)
Target: Histamine Receptor
Betahistine dihydrochloride
Cat.No: T0246
Synonym: PT-9,Betahistine 2HCl,盐酸倍他司汀
Target: Histamine Receptor
Irdabisant
Cat.No: T32191
Synonym: CEP-26401,CEP 26401,CEP26401
Target: Histamine Receptor
LML134
Cat.No: T8514
Synonym: LML-134
Target: Histamine Receptor
Betahistine
Cat.No: T4195
Synonym: PT 9 base,倍他司汀,Vasomotal,Serc base
Target: Histamine Receptor
Mepyramine maleate
Cat.No: T1232
Synonym: 马来酸吡纳明,Pyrilamine maleate,吡拉明马来酸盐
Target: Histamine Receptor
Cipralisant
Cat.No: T14970
Synonym: GT-2331
Target: Others
MK-0249
Cat.No: T12054
Synonym:
Target: Histamine Receptor
GT-2227
Cat.No: T70112
Synonym:
Target:
GT-2394
Cat.No: T70111
Synonym:
Target:
Thioperamide
Cat.No: T23456
Synonym:
Target: Others
ZEL-H16
Cat.No: T71270
Synonym:
Target:
GSK334429
Cat.No: T27473
Synonym: GSK-334429,GSK 334429
Target:
JNJ 10181457 dihydrochloride
Cat.No: T22878
Synonym:
Target: Others
Nα-Methylhistamine dihydrochloride
Cat.No: T23038
Synonym:
Target: Others
Burimamide
Cat.No: T23841
Synonym:
Target:
NNC-38-1049
Cat.No: T28184
Synonym: NNC381049,NNC 38-1049,NNC38-1049,NNC 381049,NNC-381049
Target:
Proxyfan oxalate
Cat.No: T23190
Synonym:
Target: Others
UCL-1972
Cat.No: T29043
Synonym: UCL 1972
Target:
GT-2331
Cat.No: T69756
Synonym:
Target:
PF-03654746 Tosylate
Cat.No: T12416
Synonym:
Target: Histamine Receptor
(R)-(-)-α-Methylhistamine dihydrochloride
Cat.No: T24698
Synonym: HISTAMINE DIHYDROCHLORIDE R(-)-A-METHYL
Target:
SCH-79687
Cat.No: T69737
Synonym:
Target:
Immepip dihydrobromide
Cat.No: T22863
Synonym:
Target: Others
VUF 5681 dihydrobromide
Cat.No: T23519
Synonym:
Target: Others
Aplysamine-1
Cat.No: T26643
Synonym: Aplysamine
Target:
H3 receptor antagonist 1
Cat.No: T10911
Synonym:
Target: Histamine Receptor
(R)-(-)-α-Methylhistamine dihydrobromide
Cat.No: T12630
Synonym:
Target: Histamine Receptor
Cipralisant maleate
Cat.No: T27022
Synonym: GT-2331,Cipralisant maleate. trade name Perceptin,GT 2331,GT2331
Target:
Imetit dihydrobromide
Cat.No: T15565
Synonym: VUF 8325 dihydrobromide,SKF 91105 dihydrobromide
Target: Histamine Receptor
APD-916 dicitrate
Cat.No: T71605
Synonym:
Target:
GSK 189254 HCl
Cat.No: T19628
Synonym: GSK-189254A,GSK 189254A,GSK 189254 hydrochloride,GSK189254A
Target:
Impentamine dihydrobromide
Cat.No: T22866
Synonym:
Target: Others
Iodophenpropit dihydrobromide
Cat.No: T15590
Synonym:
Target: Histamine Receptor
Cat. No. Product Name Target Signaling Pathways
T20712 Conessine

Conessinum,Wrightine,地麻素,Roquessine,Neriine,Konessin

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Conessine (Conessinum) 是一种具有抗疟活性的甾体生物碱,是高效选择性H3 受体拮抗剂,对于人、狗、豚鼠和大鼠 H3受体的Ki 分别为 5.4、6.0、5.7 和 25 nM。

天然产物

Conessine
Cat.No: T20712
Synonym: Conessinum,Wrightine,地麻素,Roquessine,Neriine,Konessin
Target: Histamine Receptor
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