T23513
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AChR
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VU10010 (VU 10010) 是一种高度选择性的M4mAChR 变构增强剂,EC50为 400 nM。它与 M4mAChR 的变构位点结合,增强与 G 蛋白偶联,增加对乙酰胆碱的亲和力,还会增加卡巴胆碱引起的兴奋性传导抑制。 |
T23310
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5-HT Receptor
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SB 203186 hydrochloride 是一种选择性的、竞争性的5-HT4拮抗剂。它拮抗5-HT4受体介导的多巴酚收缩大鼠离体食管弛缓,其在大鼠食管、豚鼠回肠和人类结肠的 pKB 值分别是 10.9、9.5 和 9.0。 |
TP2209L
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IGF-1R
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Xenin 8 acetate 是神经降压素/异视素家族中 Xenin 的生物活性片段。 Xenin 8 acetate 增强精氨酸诱导的胰岛素释放(40%)并增强胰高血糖素对精氨酸(60%)和卡巴胆碱(50%)的反应。 |
T67956L
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5-HT Receptor
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Litoxetine HCl 是一种选择性5-羟色胺(5-HT)再摄取抑制剂(SSRI)和混合5-羟色胺拮抗剂,可用于治疗尿失禁。Litoxetine HCl 在没有抗毒蕈碱特性的浓度下(10 nM-1 microM)引起大鼠离体食道肌肉粘膜的浓度依赖性松弛,使卡巴胆碱张力降低达37%,更高浓度的Litoxetine HCl(3微摩-300微摩)与明显的松弛有关,直至取消卡巴胆碱张力。以前在离体豚鼠肠道中证明的利托西汀的抗心律失常活性,在浓度大于1 microM 时在大鼠离体食道肌肉粘膜中发挥了作用。 Litoxetine HCl 的5-HT 释放作用可以解释利托西汀对未处理的大鼠组织中的5-HT 诱导的松弛的效力,这种效力被pCPA 处理所逆转。 |
T16686
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TRP/TRPV Channel
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Pyr10 是吡唑衍生物,是TRPC3通道的选择性抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的 HEK293 细胞中的 Ca2+流入。它具有区分受体操纵的TRPC3和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。 |
T67959
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Thrombin
Serine Protease
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Pirodomast 是血栓素 A(TXA2)合成酶抑制剂。Pirodomast 能抑制白三烯(LT)D4、C4、E4 的形成和血栓素 B2(TXB2)的活性,但对组胺、甲氧胆碱、血清素、LTC4 或血小板活化因子诱导的豚鼠支气管痉挛的拮抗作用较弱或无效。Pirodomast 在体外对豚鼠气管只有微弱的松弛活性。Pirodomast 是一种潜在的抗过敏化合物,在体外可抑制胰蛋白酶的蛋白水解活性,在体内可阻止抗原诱发过敏绵羊的即时和晚期哮喘反应,抑制抗原诱导的过敏绵羊对组胺和卡巴胆碱的气道高反应性。 |
T34958
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TRK-380 (TAC-301) is an effective and selective β3-adrenergic receptor agonist. TRK-380 improves formalin-induced frequent urination in rats and carbachol-induced bladder contraction in dogs (a decrease of 37.6%). |
T61529
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Pirmenol hydrochloride 通过阻断毒蕈碱性受体来抑制IK.ACh。Pirmenol 抑制 Carbachol 诱导的 IK.ACh,IC50值为 0.1 μM。 |
T61309
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(R)-Oxybutynin (Aroxybutynin) is an orally active muscarinic receptor antagonist, which exhibits antimuscarinic, antispasmodic, and anticholinergic activity. This compound, being the (R)-isomer of Oxybutynin, competitively antagonizes Carbachol-induced contractions. It is particularly useful in researching neurogenic bladder dysfunction-related incontinence [1] [2] [3]. |
T37718
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Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and mechanical stimulation in a rat model of carrageenin-induced inflammation when administered at a dose of 2 nmol injected into the nucleus accumbens.[3][4] Galanin (5 μg, i.c.v.) also inhibits acetylcholine release induced by scopolamine in the ventral hippocampus of freely moving rats. [5] |