Motilin (26-47), human, porcine

Names

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

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

Biological Activity

[Description]:

Motilin(human, porcine) is an endogenous motilin receptor ligand with Ki and EC50 of 2.3 nM and 0.3 nM in a Chinese hamster ovary cell line.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Motilin Receptor

Research Areas >> Others

Peptides

[Target]

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

[In Vitro]

[Bpa1,Ile13]motilin is a full agonist at the motilin receptor that increases intracellular calcium in a concentration-dependent manner (EC50 = 1.5 ± 0.4 nM)[1]. Motilin binds with high affinity (IC50 0.7± 0.2 nM) to receptors on smooth muscle cells. Motilin selectively activates G(q) and G(13), stimulates G alpha(q)-dependent phosphoinositide (PI) hydrolysis and 1,4,5-trisphosphate (IP(3))-dependent Ca2+ release, and increases cytosolic free Ca2+. Motilin induces a biphasic, concentration-dependent contraction (EC50 = 1.0 +/- 0.2 nM), consisting of an initial peak followed by a sustained contraction[2].

[References]

[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.

[Related Small Molecules]

GSK962040

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₂₀H₁₈₈N₃₄O₃₅S

[ Molecular Weight ]:
2699.05000

[ Exact Mass ]:
2697.37000

[ PSA ]:
1191.49000

[ LogP ]:
4.75460

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

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.