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胃动素

胃动素用途

Motilin(human, porcine) 是一种内源性的 motilin 受体激动剂，在中国仓鼠卵巢细胞中，K_i 值和 EC₅₀ 值分别为 2.3 nM 和 0.3 nM。

胃动素名称

[ CAS 号 ]:
52906-92-0

[ 中文名 ]:
胃动素

[ 英文名 ]:
Motilin (26-47), human, porcine

[英文别名 ]:

Motilin (26-47), human, porcine

胃动素生物活性

[ 描述 ]:

Motilin(human, porcine) 是一种内源性的 motilin 受体激动剂,在中国仓鼠卵巢细胞中,Ki 值和 EC50 值分别为 2.3 nM 和 0.3 nM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> Motilin Receptor

研究领域 >> 其他

多肽产品

[ 靶点 ]

EC50: 0.3 nM (motilin receptor, Chinese hamster ovary cell)[1] Ki: 2.3 nM (motilin receptor, Chinese hamster ovary cell)[1]

[体外研究]

[Bpa1,Ile13]胃动素是胃动素受体的完全激动剂,以浓度依赖性方式增加细胞内钙(EC50 = 1.5±0.4 nM)[1]。胃动素以高亲和力(IC50 0.7±0.2 nM)与平滑肌细胞上的受体结合。 Motilin选择性激活G(q)和G(13),刺激Gα(q)依赖性磷酸肌醇(PI)水解和1,4,5-三磷酸(IP(3))-依赖性Ca2 +释放,并增加细胞内游离Ca2 + 。胃动素诱导双相,浓度依赖性收缩(EC50 = 1.0 +/- 0.2 nM),包括初始峰值,然后是持续收缩[2]。

[参考文献]

[1]. Coulie B, et al. Identification of peptide ligand-binding domains within the human motilin receptor using photoaffinity labeling. J Biol Chem. 2001 Sep 21;276(38):35518-22. Epub 2001 Jul 18.

[2]. Huang J, et al. Signaling pathways mediating gastrointestinal smooth muscle contraction and MLC20 phosphorylation by motilin receptors. Am J Physiol Gastrointest Liver Physiol. 2005 Jan;288(1):G23-31.

[相关活性小分子]

Camicinal

胃动素物理化学性质

[ 分子式 ]:
C₁₂₀H₁₈₈N₃₄O₃₅S

[ 分子量 ]:
2699.05000

[ 精确质量 ]:
2697.37000

[ PSA ]:
1191.49000

[ LogP ]:
4.75460

胃动素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

胃动素文献

Heterotrimeric guanosine triphosphate-binding protein-coupled modulatory actions of motilin on K+ channels and postsynaptic γ-aminobutyric acid receptors in mouse medial vestibular nuclear neurons.

Eur. J. Neurosci. 37(3) , 339-50, (2013)

Some central nervous system neurons express receptors of gastrointestinal hormones, but their pharmacological actions are not well known. Previous anatomical and unit recording studies suggest that a ...

Gastrointestinal dysmotility: evidence and clinical management.

Curr. Opin. Clin. Nutr. Metab. Care 16(2) , 209-16, (2013)

Gastrointestinal dysmotility and dysfunction underlie our difficulties in providing adequate nutrition by the enteral route to our critically ill patients.Recent studies have quantified gastric emptyi...

Effects of intrathecal opioids combined with low-dose naloxone on motilin and its receptor in a rat model of postoperative pain

Life Sci. 103(2) , 88-94, (2014)

Aims To investigate the effects of intrathecal morphine and fentanyl combined with low-dose naloxone on the expression of motilin and its receptor in a rat model of postoperative pain.

更多文献

胃动素

胃动素用途

胃动素名称

胃动素生物活性

胃动素物理化学性质

胃动素安全信息

胃动素文献

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