T60577
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Cycrimine 是毒蕈碱胆碱能受体(mAChR)M1的口服活性拮抗剂,可降低帕金森模型中乙酰胆碱的水平。Cycrimine 具有解痉活性,可用于研究行为和精神障碍。 |
T76342
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α-Conotoxin M I 是 mAChR 和α1β1γδnAChR 的选择性和有效的抑制剂,但对尼古丁刺激的多巴胺释放无影响。α-Conotoxin 毒素是一种小的、富含二硫的多肽,竞争性地抑制肌肉和神经元的尼古丁 AChR。 |
T37801
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rac-Desethyl oxybutynin is an active metabolite of the muscarinic acetylcholine receptor (mAChR) antagonist oxybutynin .1,2,3rac-Desethyl oxybutynin is formed from oxybutynin by the cytochrome P450 (CYP) isoform CYP3A4.2It binds to mAChRs in isolated rat bladder, submaxillary gland, heart, and colon with Kivalues of 5.38, 3.12, 16, and 5.59 nM, respectively.rac-Desethyl oxybutynin (0.4 and 0.8 mg/kg) reduces micturition pressure in rats.3 |
T75587
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Dendroaspis Viridis Venom (Western Green Mamba Venom) 是从 Dendroaspis Viridis (绿曼巴蛇) 提取的蛇毒,其中含有多种毒蕈碱毒素亚型,这些亚型靶向不同的毒蕈碱受体 (mAChR)。该毒液是一种由小分子和多肽/蛋白质组成的复杂混合物,显示出神经毒性、细胞毒性、心脏毒性、肌肉毒性以及多种酶活性。进一步研究表明,这些毒素具有抗肿瘤、抗菌、抗凝和镇痛的潜在活性。 |
T40161
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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, also known as (Rac)-Desfesoterodine hydrochloride, is an active metabolite of Tolterodine that functions as a mAChR antagonist. It exhibits significant affinity (K i values) for M1, M2, M3, M4, and M5 receptors, with values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This compound is commonly employed in research related to overactive bladder conditions. |
T60253
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(±)-Muscarine chloride 是 Muscarine chloride 的外消旋体。Muscarine 是一种原型毒蕈碱乙酰胆碱受体 (mAChR) 激动剂。 |
T79618
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M3/PDE4 modulator-1 (10f) 为多功能化合物,具备M3mAChR拮抗和PDE4抑制作用。于OVA大鼠模型中,M3/PDE4 modulator-1 (10-1000 nM/kg;iv) 能降低半胱氨酸嗜酸性粒细胞内流。 |
T74988
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DIBA-Cy5 是一种 DIBA 荧光拮抗剂,由 DIBA-炔结合 Cyanine5 荧光团 (Cy5) 和聚乙二醇 (PEG) 生物分子组成。DIBA-Cy5 可以作为荧光配体,适合通过点击化学附着探针。DIBA-Cy5 对 type-2mAChR(M2R) 具有很高的结合亲和力 ( Kd=1.80 nM),可直接染色小鼠窦房结的 M2R 受体。 |
T33950
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PF-06767832 is a high quality M1 selective PAM (M1 PAM EC50 = 60 nM; M2-M5 PAM EC50 > 10 microM; CNS MPO = 4.9). PF-06767832 has well aligned physicochemical properties, good brain penetration and pharmacokinetic properties. Extensive safety profiling |
T73272
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VU6019650 是一种强效、选择性的M5mAChR 正向拮抗剂 (IC50=36 nM),能够用于减轻阿片类药物使用障碍 (OUD) 的研究。VU6019650 具有血脑透过性,可能调节中边缘多巴胺能奖赏回路。VU6019650 能够阻断Oxotremorine M iodide 诱导引起的腹侧被盖区中脑 (VTA) 多巴胺神经元的放电速率的增加。 |