Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9889 |
M4 mAChR agonist-1
4-Piperidinecarboxamide, 1-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)- |
AChR | Neuroscience |
M4 mAChR agonist-1 (4-Piperidinecarboxamide, 1-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)-) 是一种有效的 M4 mAChR 激动剂(EC50 >10 μM)。 | |||
T4494 |
CLOZAPINE N-OXIDE
氯氮平N-氧化,氯氮平N-氧化物 |
Dopamine Receptor; 5-HT Receptor; AChR; Drug Metabolite | GPCR/G Protein; Metabolism; Neuroscience |
Clozapine N-oxide 是 Clozapine 的主要代谢产物,具有血脑屏障渗透性。Clozapine N-oxide 是一种 DREADDs 激动剂,可激活 DREADD 受体 hM3Dq 和 hM4Di。Clozapine N-oxide 也是一种多巴胺拮抗剂和选择性毒蕈碱 M4 受体激动剂。 | |||
T81893 | M1/M4 muscarinic agonist 2 | ||
M1/M4 muscarinic antagonist 2(compound 40)为选择性抑制M1与M4受体的化合物,其IC50值分别为19 nM和42 nM。 | |||
T6575 |
LY2119620
|
AChR | Neuroscience |
LY2119620 是人 M2 和 M4 毒蕈碱乙酰胆碱受体的特异性变构激动剂。 | |||
T9694 |
Emraclidine
CVL-231 |
AChR | Neuroscience |
Emraclidine (CVL-231) 是一种毒蕈碱 M4 受体阳性变构调节剂,可用于神经系统疾病研究。 | |||
T23297 |
(S)-(+)-Dimethindene maleate
|
AChR; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
(S)-(+)-Dimethindene maleate 是一种可口服且具有选择性毒蕈碱 M2 受体和组胺 H1 受体拮抗剂,抑制毒蕈碱 M1,M3 和 M4 受体。 | |||
T17244 |
VU0467154
|
AChR | Neuroscience |
VU0467154 是 M4 毒蕈碱的乙酰胆碱受体的正向调节剂,能够增强小鼠、人和食蟹猴 M4 受体对乙酰胆碱的反应,pEC50值分别为 7.75、6.2 和 6。 | |||
T8219 |
VU0238441
|
AChR | Neuroscience |
VU0238441是一种泛毒蕈碱型乙酰胆碱受体阳性变构调节剂,对 M1、M2、M3、M5 和 M4 的EC50分别为 3.2、2.8、2.2、2.1 和大于 10 μM。 | |||
T0862 |
Diphenidol hydrochloride
Diphenidol HCl,盐酸地芬尼多,Difenidol hydrochloride |
Sodium Channel; AChR | Membrane transporter/Ion channel; Neuroscience |
Diphenidol hydrochloride (Difenidol hydrochloride) 是一种非选择性的毒蕈碱 M1-M4 受体拮抗剂,具有抗心律失常活性,用作抗眩晕药和止吐药。它也是神经细胞电压门控离子通道的有效非特异性阻滞剂。 | |||
T1475 |
Fesoterodine fumarate
Toviaz,SPM 907,富马酸非索罗定 |
AChR | Neuroscience |
Fesoterodine fumarate (Toviaz) 是可口服的,非亚型选择性的竞争性毒蕈碱受体拮抗剂,用于膀胱过度活动症,对 M1、M2、M3、M4 和 M5 受体的pKi 值分别为 8.0、7.7、7.4、7.3 和 7.5。 | |||
T1281 |
Tropicamide
Ro 1-7683,托吡卡胺 |
AChR | Neuroscience |
Tropicamide (Ro 1-7683) 是一种选择性的 M4毒蕈碱乙酰胆碱受体拮抗剂,作为滴眼剂使用时,会产生短效瞳孔扩张和睫状肌麻痹。 | |||
T23124 |
PD 102807
|
Others | Others |
M4 muscarinic receptor antagonist | |||
T13924 | Thiochrome | Others | Others |
Thiochrome is a selective enhancer of M4 muscarinic receptor of acetylcholine (ACh) affinity. | |||
T39543 |
VU6000918
|
||
VU6000918 is a positive allosteric modulator that targets the muscarinic acetylcholine receptor subtype M4. It exhibits a half maximal effective concentration (EC50) of 19 nM for the human M4 receptor. | |||
T17245 |
VU0467485
AZ13713945 |
Others | Others |
VU0467485 is a potent and selective muscarinic acetylcholine receptor 4 positive allosteric modulator. VU0467485 potentiates the activity of ACh at M4 (EC50s: 26.6 nM and 78.8 nM at the rat and human M4 receptors, respectively). VU0467485 displays selecti | |||
T13322 |
VU6005806
AZN-00016130 |
Others | Others |
VU6005806 is a potent positive allosteric modulator (PAM) of muscarinic acetylcholine receptor subtype 4 (M4) (EC50s: 94 nM, 28 nM, 87 nM, and 68 nM for human, rat, dog, and cyno M4, respectively), and used in the study of neuropsychiatric disorders. | |||
T39010 |
Xanomeline tartrate
LY 246708 tartrate,Xanomeline tartrate |
||
Xanomeline (LY 246708), a potent agonist of muscarinic M1/M4 receptors, exhibits antipsychotic-like activity and enhances neuronal excitability. It is a valuable compound for studying schizophrenia. | |||
T36662 |
Imidafenacin Metabolite M4
Imidafenacin Metabolite M4 |
||
Imidafenacin metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist imidafenacin.1It is formed from imidafenacin by the cytochrome P450 (CYP) isoform CYP3A4. 1.Kanayama, N., Kanari, C., Masuda, Y., et al.Drug-drug interactions in the metabolism of imidafenacin: Role of the human cytochrome P450 enzymes and UDP-glucuronic acid transferases, and potential of imidafenacin to inhibit human cytochrome P450 enzymesXenobiotica37(2)139-154(2007) | |||
T23763 |
Atropine Oxide
NSC 72861,NSC72861,NSC-72861 |
||
Atropine Oxide is a derivative of Atropine. Atropine is a competitive antagonist of the muscarinic acetylcholine receptor types M1, M2, M3, M4, and M5. Atropine is a medication to treat certain types of nerve agents and pesticide poisonings as well as som | |||
T37728 | Methoctramine (hydrate) | ||
Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs wit... | |||
T16443 |
PCS1055 dihydrochloride
|
Others | Others |
PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res | |||
T39545 | MK-6884 | ||
MK-6884, a positive allosteric modulator (PAM) of M4 muscarinic receptors, exhibits a high affinity (Ki = 0.19 nM). It is a valuable compound for the investigation of neurodegenerative diseases. Additionally, MK-6884 can be efficiently radiolabeled with carbon-11, enabling its use as a PET imaging agent. | |||
T69232 | Atropine Oxide Hydrochloride | ||
Atropine Oxide is a derivative of Atropine. Atropine is a medication to treat certain types of nerve agent and pesticide poisonings as well as some types of slow heart rate and to decrease saliva production during surgery. Atropine is a competitive antagonist of the muscarinic acetylcholine receptor types M1, M2, M3, M4 and M5. It is classified as an anticholinergic drug (parasympatholytic). | |||
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。 | |||
T74709 | LAS190792 | ||
LAS190792 (AZD8999) 是一种毒蕈碱 (muscarinic) 拮抗剂及β2-肾上腺素能受体 (β2-adrenoceptor) 激动剂,其pIC50值针对 M1, M2, M3, M4, M5, β1, β2, β3 分别为 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6。该化合物作为支气管扩张剂具有应用潜力。 | |||
T71963 |
(−)-WIN 55,212-3 mesylate
|
||
(−)-WIN 55,212-3 mesylate is an aminoalkylindole derivative which acts as a competitive neutral antagonist of the human cannabinoid CB2 receptor, blocking both the stimulating action of CP 55,940 and the inverse agonism of SR 144528. (−)-WIN 55,212-3 neither antagonizes nor mimics the effects of Δ9-THC on rat cerebellar membranes, which presumably express the CB1 receptor. (−)-WIN 55,212-3 also weakly antagonizes the melatonin MT1 and muscarinic M4 receptors but has no effect on several other G ... | |||
T36241 |
Arecaidine propargyl ester (hydrobromide)
|
||
Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecai... |