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Motilin receptor agonists and antagonists act on the receptor for motilin, a gut peptide hormone. Motilin is a 22-amino acid peptide released from endocrine cells of the upper small intestine. Its periodic release starts phase III of the migrating motor complex, a band of contractions that sweeps the empty stomach and gut. The motilin receptor (MLNR), previously known as G protein-coupled receptor 38 (GPR38), was identified in 1999 as a G protein-coupled receptor of the human gastrointestinal tract. Agonists derived from macrolide antibiotics, called motilides, act on the same receptor. The category holds Motilin, human, porcine and Motilin, canine, the small-molecule agonist camicinal and the motilide EM-523. MA-2029 and ANQ-11125 are listed as antagonists that block motilin-induced responses.
Synonyms: GSK962040 hydrochloride; GSK-962040
Camicinal hydrochloride (GSK962040 hydrochloride) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.
Synonyms: GSK962040
Camicinal (GSK962040) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.
Motilin (26-47), human, porcine is a potent agonist of the motilin receptor, exhibiting a Ki value of 2.3 nM and an EC50 of 0.3 nM in a Chinese hamster ovary cell line. This peptide plays a critical role in gastrointestinal motility and is instrumental in research focused on digestive system disorders and hormone signaling pathways. Its application extends to various studies involving gut motility regulation and the therapeutic potential of motilin-related compounds.
Synonyms: Motilin (canine)
Motilin, canine is a 22-amino acid peptide that acts as a potent agonist of gastrointestinal smooth muscle contraction. This bioactive peptide plays a crucial role in stimulating intestinal motility and has potential applications in gastrointestinal research. It is primarily used to study motility disorders and the regulation of digestive processes in canine models.
KC-11458 is a motilin agonist that enhances gastric motility by stimulating motilin receptors in the gastrointestinal tract. This compound is primarily used for research into gastrointestinal motility disorders and can be valuable in studies investigating the regulation of gastric emptying processes. Its ability to accelerate gastric emptying makes it a potential tool for exploring therapeutic targets in digestive disorders.
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EM-523 is a motilin agonist and an erythromycin derivative that selectively targets motilin receptors. It has demonstrated biological activity with pED50 values of 8.19 and 6.08 for inducing contractions in rabbit small intestinal tissue and human duodenal tissue, respectively. This compound is valuable for investigating gastrointestinal diseases and advancing research related to motility disorders.
Synonyms: GM 611 fumarate
Mitemcinal fumarate is a selective agonist of the motilin receptor. It demonstrates significant biological activity in promoting defecation and increasing stool bulk without causing excessive diarrhea, as evidenced in preclinical studies in rabbits and dogs. Its rapid onset and short duration of action suggest potential applications in the treatment of constipation, making it a valuable compound for gastrointestinal research.
Synonyms: GM 611
Mitemcinal is an oral motilin receptor agonist, specifically targeting motilin pathways to enhance gastrointestinal motility. Research demonstrates its capability to promote defecation in animal models, such as rabbits and dogs, without inducing severe diarrhea. Additionally, Mitemcinal increases stool weight while maintaining water content and reduces the latency to first defecation in dogs. This makes Mitemcinal a promising candidate for studies on constipation management and gastrointestinal disorders.
EM574 is a potent agonist of the motilin receptor, demonstrating significant activity in the human gastric antrum and rabbit gastrointestinal tract in vitro. As an erythromycin derivative, EM574 is utilized in research applications exploring gastrointestinal motility and related disorders. Its ability to selectively modulate motilin receptor signaling makes it a valuable tool for advancing studies in gastrointestinal physiology and pharmacology.
![[Nle13]-Motilin](https://www.adooq.com/media/catalog/product/cache/16359f9c8ddfa823fcb5503b1e11b7ae/a/6/a61952-nle13-motilin.gif)
[Nle13]-Motilin is a synthetic analog of motilin that functions as a motilin receptor agonist. It effectively stimulates gastrointestinal motility by activating the motilin receptor, making it a valuable tool in studies related to gastrointestinal physiology and potential therapeutics for gut motility disorders. Research applications include investigations into the modulation of gastric emptying and the treatment of gastrointestinal dysmotility.
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Synonyms: OHM 11638; BAX-ACC 1638; MOT 288
Atilmotin is a selective motilin receptor agonist with a pKd value of 8.94. It enhances gastrointestinal motility by increasing lower esophageal sphincter (LES) and gastric pressures, making it a valuable tool for studying esophageal and gastric motility. This compound is particularly relevant for research applications focused on gastrointestinal disorders and the development of prokinetic agents.
