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阿拉丁小分子抑制剂、激动剂、拮抗剂---神经信号通路（下）
神经信号
神经信号参与中枢神经系统的结构、功能、遗传和生理的调节。神经元合成/导入神经递质，并将其储存在突触前囊泡中。突触前神经元释放的小泡，进而传递神经冲动。常见的神经递质有γ氨基丁酸（GABA）、谷氨酸、血清素、多巴胺等。在神经信号通路中，这些神经递质的功能障碍可能多种神经系统疾病，如慢性疼痛、神经退行性疾病、失眠、精神障碍（精神分裂症、双相情感障碍、抑郁症和成瘾）等。
神经信号通路转导过程
当受到来自环境或其他神经元的信号刺激时，神经递质受体通过G蛋白偶联信号通路和G蛋白非依赖机制激活下游细胞内信号通路：包括cAMP/PKA, PI3K/AKT, 磷脂酶A2（PLA2）, 磷脂酶C（PLC）信号通路等。例如，多巴胺受体通过cAMP激活PKA等信号分子，通过CREB和其他转录因子的作用调控基因表达。其他神经递质如NMDAR或AMPAR与控制Ca2+和Na+流量的离子通道有关，这样就能在突触后神经元中传递动作电位。
神经信号通路图
产品列表
*多巴胺受体
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | Ki | pKi | EC50 |
|---|---|---|---|---|---|---|---|---|---|
| B129216 | Benztropine mesylate | ≥98% | 132-17-2 | 1g,5g | DAT | 118 nM | |||
| C129569 | 盐酸氯丙嗪 | 分析标准品 | 69-09-0 | 250mg | |||||
| C131611 | 盐酸氯丙嗪 | ≥98%(HPLC) | 69-09-0 | 5g,25g,100g | |||||
| B129446 | Amfebutamone (Bupropion) HCl | ≥98% (HPLC) | 31677-93-7 | 250mg,1g,5g | Dopamine receptor | ||||
| T162449 | 三氟拉嗪二盐酸盐 | >98.0%(HPLC)(T) | 440-17-5 | 5g,25g,100g | Dopamine D2 receptor | 1.1 nM | |||
| D129436 | Domperidone | ≥98% | 57808-66-9 | 50mg,250mg,1g,5g,25g,100g | Dopamine D2 receptor | ||||
| O126519 | Olanzapine | ≥99% | 132539-06-1 | 1g,5g | 5-HT2 | ||||
| D2 receptor | |||||||||
| Q129431 | Quetiapine Fumarate | ≥98% | 111974-72-2 | 1g,5g,10g,25g | Dopamine receptor | ||||
| Histamine receptor | |||||||||
| Adrenergic Receptor | |||||||||
| E129717 | Ziprasidone HCl | ≥98% | 122883-93-6 | 250mg,1g | 5-HT receptor | ||||
| Dopamine receptor | |||||||||
| M124438 | 甲氧氯普胺 | 98% | 364-62-5 | 5g,25g | Dopamine receptor | ||||
| A129432 | Amisulpride | ≥98% | 71675-85-9 | 50mg,250mg,1g | Dopamine receptor | ||||
| P120141 | 帕利哌酮 | 98% | 144598-75-4 | 10mg,50mg,250mg,1g,5g,25g | Dopamine receptor | ||||
| H113852 | 氟哌啶醇 | 98% | 52-86-8 | 5g,25g | |||||
| C129441 | Chlorprothixene | ≥98% | 113-59-7 | 50mg,250mg | D1 | 18nM | |||
| D2 | 2.96 nM | ||||||||
| D3 | 4.56 nM | ||||||||
| D5 | 9 nM | ||||||||
| H1 | 3.75 nM | ||||||||
| 5-HT2 | 9.4 nM | ||||||||
| 5-HT6 | 3 nM和 | ||||||||
| 5-HT7 | 5.6 nM | ||||||||
| P108681 | 吩噻嗪 | 98% | 92-84-2 | 250mg,100g,500g,5kg | D2 receptor | ||||
| D129475 | Droperidol | ≥98% | 548-73-2 | 50mg,250mg,1g | |||||
| L129452 | Levosulpiride | ≥98% | 23672-07-3 | 5g,25g | D2 receptor | ||||
| T101542 | 延胡索乙素 | 分析标准品,>97% | 2934-97-6 | 250mg,1g,5g | |||||
| P160649 | Perphenazine | >97.0% | 58-39-9 | 1g,5g,25g | |||||
| H197233 | 6-羟基多巴胺氢溴酸盐 | 95% | 636-00-0 | 50mg,250mg,1g | |||||
| C171261 | Chlorprothixene hydrochloride | - | 6469-93-8 | 1g | |||||
| T162447 | 三氟丙嗪盐酸盐 | >98.0%(HPLC) | 1098-60-8 | 1g,5g | |||||
| P160772 | Penfluridol | >97.0%(HPLC) | 26864-56-2 | 200mg,1g | |||||
| M132784 | Molindone Hydrochloride | ≥98.0%(HPLC) | 15622-65-8 | 100mg,250mg,1g,5g,25g | D2 receptor | ||||
| D5 receptor | |||||||||
| R136626 | Rotundine | ≥98% | 483-14-7 | 100mg,250mg,500mg | |||||
| P160775 | (±)-Sulpiride | >98.0%(HPLC) | 15676-16-1 | 5g,25g,100g | D2 receptor | ||||
| T135203 | 丁苯那嗪 | 98% | 58-46-8 | 250mg,1g,5g | |||||
| A129598 | Azaperone | ≥99% | 1649-18-9 | 50mg,250mg | Dopamine receptor | ||||
| C184839 | Chlorpromazine | 95% | 50-53-3 | 1g,5g | |||||
| C171931 | Cariprazine hydrochloride | 97% | 1083076-69-0 | 1g | dopamine D2/D3 receptor | ||||
| D111048 | 左旋多巴 | 99% | 59-92-7 | 25g,100g,500g | Dopamine receptor | ||||
| D111049 | 左旋多巴 | 分析标准品,>99% | 59-92-7 | 20mg | Dopamine receptor | ||||
| A109736 | 盐酸金刚烷胺 | 99%（T） | 665-66-7 | 5g,25g,100g,500g | Dopamine receptor | ||||
| P129443 | Pramipexole 2HCl Monohydrate | ≥98%(HPLC) | 191217-81-9 | 50mg,250mg,1g | D2S Receptor | 3.9 nM | |||
| D2L Receptor | 2.2 nM | ||||||||
| D3 receptor | 0.5 nM | ||||||||
| D4 receptor | 5.1 nM | ||||||||
| P129434 | Pramipexole | ≥99% | 104632-26-0 | 10mg,50mg | D2S Receptor | 3.9 nM | |||
| D2L Receptor | 2.2 nM | ||||||||
| D3 receptor | 0.5 nM | ||||||||
| D4 receptor | 5.1 nM | ||||||||
| P129456 | Pergolide mesylate | ≥99% | 66104-23-2 | 2.5mg | |||||
| B178171 | brexpiprazole | 97% | 913611-97-9 | 1g | 5-HT1A | 0.12 nM | |||
| human noradrenergic α1B | 0.17 nM | ||||||||
| Dopamine D2L | 0.3 nM | ||||||||
| 5-HT2A receptors | 0.47 nM | ||||||||
| α2C receptors | 0.59 nM | ||||||||
| P160771 | 吡贝地尔 | >98.0%(GC)(T) | 3605-01-4 | 200mg,1g | adrenoceptor α2C | 7.2 | |||
| adrenoceptor α2A | 7.1 | ||||||||
| D2 receptor | 6.9 | ||||||||
| P129442 | PD128907 HCl | ≥98% | 112960-16-4 | 5mg,25mg,100mg | D3 receptor | 0.64 nM | |||
| R126364 | Rotigotine | ≥98% | 99755-59-6 | 10mg,50mg | Dopamine receptor | ||||
| P165634 | Pramipexole dihydrochloride | >98% (HPLC) | 104632-25-9 | 10mg,50mg | D2S受体 | 3.9 nM | |||
| D2L受体 | 2.2 nM | ||||||||
| D3受体 | 0.5 nM | ||||||||
| D4受体 | 5.1 nM | ||||||||
| M132847 | 1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐 | ≥98% | 23007-85-4 | 25mg,100mg | |||||
| O101521 | 章胺盐酸盐 | 98% | 770-05-8 | 1g,5g |
*阿片受体
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | Ki |
|---|---|---|---|---|---|---|---|
| R126180 | Racecadotril | ≥98% | 81110-73-8 | 250mg,1g,5g,25g | Opioid receptor | 4.5 μM | |
| N129470 | Naloxone HCl | ≥99% | 357-08-4 | 50mg,250mg,1g | Opioid receptor | ||
| J125889 | JTC-801 | ≥99% | 244218-51-7 | 5mg,10mg,50mg | Opioid receptor-like1 (ORL1) | 94 nM | |
| N129470 | Naloxone HCl | ≥99% | 357-08-4 | 50mg,250mg,1g | Opioid receptor | 8 nM | |
| A124975 | Alvimopan | ≥98% | 156053-89-3 | 5mg,25mg,100mg | μ-opioid receptor | 0.77 nM | |
| δ-opioid receptor | 4.4 nM | ||||||
| κ-opioid receptor | 40 nM | ||||||
| L129465 | Loperamide HCl | ≥98% | 34552-83-5 | 5g,25g | μ-opioid receptor | 3.3 nM | |
| δ-opioid receptor | 48 nM | ||||||
| A127848 | ADL5859 HCl | ≥98% | 850173-95-4 | 5mg,10mg,50mg | δ-opioid receptor | 0.8 nM | |
| M109802 | 苦参碱 | 分析标准品,≥98% | 519-02-8 | 20mg | κ-opioid receptor | ||
| M109803 | 苦参碱 | 98% | 519-02-8 | 100mg,1g,5g,25g | κ-opioid receptor | ||
| T129468 | Trimebutine | ≥98% | 39133-31-8 | 250mg,5g,25g,100g | μ-opiate receptor | ||
| κ-opioid receptor | |||||||
| delta-opiate receptor | |||||||
| M129400 | Meptazinol HCl | ≥99% | 59263-76-2 | 10mg,50mg,250mg | opioid receptor | 58nM | |
| A106730 | 双(2-乙己基)磺基丁二酸钠 | 96% | 577-11-7 | 25g,100g,500g |
*GABA受体
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | Ki | EC50 |
|---|---|---|---|---|---|---|---|---|
| S161023 | 2-丙戊酸钠 | ≥98.0% | 1069-66-5 | 5g,25g,100g,500g | HDAC | |||
| N129597 | 尼氟酸 | >98.0%(HPLC) | 4394-00-7 | 1g,5g,25g,100g | COX-2 | |||
| GABA receptor | ||||||||
| T134804 | Tiagabine hydrochloride | ≥98%(HPLC) | 145821-59-6 | 10mg,50mg,250mg | GABA uptake | |||
| N129604 | Nefiracetam | ≥98% | 77191-36-7 | 50mg,250mg,1g | GABA receptor | |||
| F124794 | Flumazenil | >99% (HPLC) | 78755-81-4 | 25mg,100mg,500mg | GABAA receptor | |||
| I134619 | 咪唑-4-乙酸盐酸盐 | 97% | 3251-69-2 | 1g,5g | GABAC receptors | |||
| B110235 | 右旋比扣扣灵碱 | 分析标准品 | 485-49-4 | 20mg | GABAA receptor | 2 μM | ||
| B110236 | 右旋比扣扣灵碱 | 98% | 485-49-4 | 25mg,100mg,500mg | GABAA receptor | 2 μM | ||
| G109811 | 银杏内酯 A | ≥98% | 15291-75-5 | 10mg,50mg | GABA receptor | 14.5 μM | ||
| P103065 | 戊四唑 | 98% | 54-95-5 | 5g,25g | GABA receptor | |||
| M129572 | Bemegride | ≥98% | 64-65-3 | 1g,10g | GABAA receptor | |||
| T162847 | 硫秋水仙苷 | >98.0%(HPLC) | 602-41-5 | 20mg | GABAA receptor | |||
| E129603 | Gabapentin HCl | ≥98% | 60142-95-2 | 10mg,50mg | GABA receptor | |||
| E129601 | Etomidate | ≥98% | 33125-97-2 | 100mg,250mg,500mg,1g,5g | GABAA receptor | |||
| G122413 | Gabapentin | 98% | 60142-96-3 | 5g,25g,100g,500g | GABA receptor | |||
| I109586 | 异哌啶酸 | 98% | 498-94-2 | 5g,25g,100g,250g,500g | GABAA receptor | |||
| B127341 | (R)-Baclofen | ≥98% | 69308-37-8 | 10mg,50mg,100mg,250mg | ||||
| P105274 | 无水哌嗪 | 99% | 110-85-0 | 100g,250g,500g,2.5kg | GABA receptor | |||
| X138043 | 巴氯酚 | ≥98.0% | 1134-47-0 | 1g,5g,25g,100g | GABAB receptor | |||
| H157351 | 6-羟基黄酮 | >98.0%(T)(HPLC) | 6665-83-4 | 1g,5g,25g | GABAA receptor | |||
| A179304 | 4-氨基-3-苯基丁酸盐酸盐 | 98% | 1078-21-3 | 5g,25g,100g | GABA receptor | |||
| B110209 | 黄芩苷 | 分析标准品,≥ 98.0 %(HPLC) | 21967-41-9 | 10mg,50mg | GABAA receptor | |||
| B110210 | 黄芩苷 | 90% | 21967-41-9 | 1g,5g,25g,100g | GABAA receptor | |||
| B110211 | 黄芩苷 | 95% | 21967-41-9 | 1g,5g | GABAA receptor | |||
| G115746 | 光甘草定 | 分析标准品,≥99% | 59870-68-7 | 20mg | α1β2γ2 | 6.3 μM | ||
| α1β3γ2 | 6.83 μM | |||||||
| α1β2 | 9.63 μM | |||||||
| α1β1γ2 | 17.23 μM | |||||||
| D299476 | 二氢杨梅素 | >97.0%(HPLC) | 27200-12-0 | 200mg,1g | ||||
| D101549 | 二氢杨梅素 | 分析标准品,≥98% | 27200-12-0 | 20mg | ||||
| H122344 | 奥拉西坦 | 97% | 62613-82-5 | 1g,5g,25g | ||||
| A104200 | γ-氨基丁酸 | 99% | 56-12-2 | 5g,25g,100g,500g | GABA receptor | |||
| A151071 | 阿坎酸钙 | >98.0%(HPLC)(N) | 77337-73-6 | 1g | ||||
| A107500 | 3-氨基丙烷磺酸 | 97% | 3687-18-1 | 1g,5g,25g,100g,500g |
*P-gp
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | Kd | Ki |
|---|---|---|---|---|---|---|---|---|
| T126671 | Tariquidar | ≥99% | 206873-63-4 | 10mg,50mg,100mg | P-gp | 5.1 nM | ||
| E126576 | Elacridar | ≥98% | 143664-11-3 | 10mg,50mg,100mg | P-gp | |||
| BCRP | ||||||||
| S117968 | 五味子乙素 | 分析标准品,>98% | 61281-37-6 | 25mg,100mg | P-gp | |||
| ATR | 7.25 μM | |||||||
| S129564 | SC144 | ≥99% | 895158-95-9 | 5mg,25mg | gp130 | |||
| L126616 | LY335979 | ≥99% | 167465-36-3 | 5mg,10mg,50mg | P-gp | 60 nM |
*P2受体
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | Ki |
|---|---|---|---|---|---|---|---|
| M129552 | MRS 2578 | ≥98% | 711019-86-2 | 10mg,50mg | P2Y6 | 37 nM | |
| T129548 | Ticlopidine HCl | ≥98% | 53885-35-1 | 1g,5g,25g | P2 receptor | ~2 μM | |
| P125739 | Prasugrel | ≥99% | 150322-43-3 | 100mg,500mg | P2Y12 receptor | ||
| T125095 | Ticagrelor | ≥98% | 274693-27-5 | 25mg,100mg,250mg,500mg,1g | P2Y12 | 2 nM | |
| A126016 | A-317491 | ≥98% | 475205-49-3 | 5mg,25mg,100mg | |||
| S129544 | Clopidogrel Bisulfate | ≥98% | 120202-66-6 | 500mg,1g,5g | P2Y12 |
*P2受体
| 项目号 | 产品名称 | 规格 | CAS | 包装 |
|---|---|---|---|---|
| A129661 | Alverine Citrate | ≥99% | 5560-59-8 | 5g,25g |
| S117970 | 五味子酯甲 | 分析标准品,>98% | 58546-56-8 | 20mg,100mg |
*MT 受体
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | Ki | pKi |
|---|---|---|---|---|---|---|---|
| R125051 | Ramelteon | ≥99% | 196597-26-9 | 10mg,50mg,100mg | MT1 receptor | 14 pM | |
| MT receptor (chicken) | 23.1 pM | ||||||
| MT2 receptor | 112 pM | ||||||
| M118674 | 褪黑素 | 98% | 73-31-4 | 250mg,1g,5g,25g,100g | melatonin receptor | ||
| T176929 | Tasimelteon | 0.97 | 609799-22-6 | 100mg | MT2 receptor | 9.8 | |
| MT1 receptor | 9.45 |
*BACE
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | EC50 |
|---|---|---|---|---|---|---|---|
| L125253 | LY2886721 | ≥99% | 1262036-50-9 | 5mg,10mg,50mg | BACE1 | 20.3 nM | |
| BACE2 | 10.2 nM | ||||||
| L128069 | LY2811376 | ≥99% | 1194044-20-6 | 5mg,10mg,50mg | BACE1 | 239 nM-249 nM | |
| Aβ | ~300 nM | ||||||
| L111134 | 马钱子苷 | 0.98 | 18524-94-2 | 10mg,50mg,100mg | AChE | 3.95 μM | |
| BChE | 33.02 μM | ||||||
| BACE1 | 47.97 μM |
*Substance P
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 |
|---|---|---|---|---|---|---|
| A125005 | Aprepitant | ≥98% | 170729-80-3 | 5mg,25mg,100mg,500mg,1g | Neurokinin-1 receptor | 0.1 nM |
*P-gp
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | Kd | Ki |
|---|---|---|---|---|---|---|---|---|
| P113899 | 盐酸普鲁卡因 | 99% | 51-05-8 | 25g,100g,500g | 5-HT3 | 1.7 μM | ||
| nAChR | 45.5 μM | |||||||
| Sodium channel | 60 μM | |||||||
| NMDA receptor | 0.296 mM | |||||||
| P113900 | 盐酸普鲁卡因 | 分析标准品 | 51-05-8 | 250mg | 5-HT3 | 1.7 μM | ||
| nAChR | 45.5 μM | |||||||
| Sodium channel | 60 μM | |||||||
| NMDA receptor | 0.296 mM | |||||||
| M129512 | (-)-MK 801 Maleate | ≥99% | 121917-57-5 | 10mg,50mg | NMDA receptor | 30.5 nM | ||
| E137445 | Eliprodil | ≥98% (HPLC) | 119431-25-3 | 10mg,50mg | NMDA | |||
| M107928 | 美金刚胺盐酸盐 | 98% | 41100-52-1 | 250mg,1g,5g,25g,100g | CYP2B6 | 0.51 nM | ||
| CYP2D6 | 94.9 μM | |||||||
| F129947 | 非氨酯 | ≥99% | 25451-15-4 | 10mg,50mg | NMDAR | 1.8 mM | ||
| L106905 | 芳樟醇 | 98% | 78-70-6 | 100ml,500ml,2.5L | NMDAR | |||
| O136159 | 奥芬那君 盐酸盐 | ≥98.0% | 341-69-5 | 1g | ||||
| K120012 | 犬尿喹啉酸 | 97% | 492-27-3 | 250mg,1g,5g | ||||
| N129532 | N-甲基-D-天冬氨酸 | ≥98% | 6384-92-5 | 100mg,250mg,1g,5g | NMDA receptor | |||
| P140270 | 吡啶-2,3-二羧酸 | 98% | 89-00-9 | 25g,100g | NMDAR | |||
| P100814 | 吡啶-2,3-二羧酸 | 99% | 89-00-9 | 25g,100g,500g | NMDAR | |||
| S102891 | 肌氨酸 | 98% | 107-97-1 | 25g,100g,250g,500g,2.5kg | ||||
| A105951 | D-天冬氨酸 | 98% | 1783-96-6 | 5g,25g,100g,250g | ||||
| M132856 | 6-甲氧基-2-萘甲酸 | ≥97.0% | 2471-70-7 | 1g,5g | NMDAR |
*Trk受体
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 细胞 | 靶点 | IC50 | Kd |
|---|---|---|---|---|---|---|---|---|
| B127174 | BMS-754807 | ≥99% | 1001350-96-4 | 5mg,10mg,50mg | 无细胞 | IGF-1R | 1.8 nM | |
| InsR | 1.7 nM | |||||||
| G129825 | GW441756 | ≥99% | 504433-23-2 | 10mg,50mg | TrkA | 2 nM | ||
| A168673 | ANA-12 | 98% (HPLC) | 219766-25-3 | 5mg,25mg | TrkB | 10 nM |
*CaMK
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | Ki | pKi |
|---|---|---|---|---|---|---|---|
| K125637 | KN-62 | ≥98% | 127191-97-3 | 5mg,25mg,100mg | CaMKⅡ | 0.9 nM | |
| P2RX7 | 15 nM | ||||||
| S107694 | 丹参酮IIA磺酸钠 | 分析标准品,≥98% | 69659-80-9 | 20mg,100mg | CYP3A4 | 6.377 μM |
*GlyT
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 |
|---|---|---|---|---|---|---|
| A129596 | Amoxapine | ≥98% | 14028-44-5 | 50mg,250mg,1g,5g | GlyT2a | 92 μM |
| GlyT1b | GlyT1b | |||||
| S102891 | 肌氨酸 | 98% | 107-97-1 | 25g,100g,250g,500g,2.5kg |
October 13, 2020
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Categories: 特色产品专题
| Tags: <a class="mp-info" href="https://mgt-en248.env.aladdin-e.com/zh_cn/blog/tag/smallmolecule">小分子</a>, <a class="mp-info" href="https://mgt-en248.env.aladdin-e.com/zh_cn/blog/tag/inhibitor">抑制剂</a>, <a class="mp-info" href="https://mgt-en248.env.aladdin-e.com/zh_cn/blog/tag/agonist">激动剂</a>, <a class="mp-info" href="https://mgt-en248.env.aladdin-e.com/zh_cn/blog/tag/antagonist">拮抗剂</a>, <a class="mp-info" href="https://mgt-en248.env.aladdin-e.com/zh_cn/blog/tag/nervesignals">神经信号</a>
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By: <a class="mp-info" href="https://mgt-en248.env.aladdin-e.com/zh_cn/blog/author/n-a">aladdin</a>
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