Page last updated: 2024-11-12

motilin

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Description

Motilin: A peptide of about 22-amino acids isolated from the DUODENUM. At low pH it inhibits gastric motor activity, whereas at high pH it has a stimulating effect. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16136567
CHEMBL ID525634
MeSH IDM0014098
PubMed CID16129683
CHEMBL ID411576
MeSH IDM0014098

Synonyms (22)

Synonym
gtpl1458
h-motilin
CHEMBL525634 ,
phe-val-pro-ile-phe-thr-tyr-gly-glu-leu-gln-arg-met-gln-glu-lys-glu-arg-asn-lys-gly-gln
9072-41-7
unii-d85v250ysi
human motilin [mi]
motilin (porcine)
motilin (human)
motilin [mi]
human motilin
d85v250ysi ,
motilin (human, porcine)
AKOS024457017
motilin porcine, >=97% (hplc)
CCA90692
bdbm50599720
motilin
bdbm50143037
chembl411576
52906-92-0
motilin (26-47), human, porcine

Research Excerpts

Overview

Motilin is a gastrointestinal hormone secreted by the duodenum. It is almost exclusively expressed in the human gastrointestinal (GI) tract. Motilin stimulates gastrointestinal motility and gallbladder emptying.

ExcerptReferenceRelevance
"Motilin is a proximal small intestinal hormone with roles in gastrointestinal motility, gallbladder emptying, and hunger initiation. "( Stimulation of motilin secretion by bile, free fatty acids, and acidification in human duodenal organoids.
Foreman, RE; George, AL; Goldspink, DA; Gribble, FM; Kay, RG; Larraufie, P; Lu, VB; Miedzybrodzka, EL; Reimann, F; Smith, CA, 2021
)
2.42
"Motilin is a gastrointestinal hormone secreted by the duodenum. "( Physiological functions and potential clinical applications of motilin.
Mori, H; Sosoranga, ER; Tanemoto, R; Verbeure, W, 2023
)
2.59
"Motilin is an endogenous peptide hormone almost exclusively expressed in the human gastrointestinal (GI) tract. "( Structural basis for motilin and erythromycin recognition by motilin receptor.
Chen, Z; Huang, S; Jiang, Y; Li, H; Li, J; Li, Z; Xu, HE; Xu, P; Xu, Y; You, C; Zhang, Y, 2023
)
2.67
"Motilin is a gastrointestinal peptide hormone that stimulates gastrointestinal motility. "( Characterization of the gastric motility response to human motilin and erythromycin in human motilin receptor-expressing transgenic mice.
Kato, S; Kawamura, T; Matsumoto, K; Matsuura, B; Shindo, M; Takahashi, A; Yoshida, A, 2019
)
2.2
"Motilin is a ghrelin-related gut peptide that induces strong contraction in the small intestine."( Age-dependent reduction of ghrelin- and motilin-induced contractile activity in the chicken gastrointestinal tract.
Kaiya, H; Kitazawa, T; Tamano, T; Teraoka, H; Yoshida, A, 2013
)
1.38
"Motilin is a gastrointestinal hormone that increases intestinal motility."( Serum motilin levels and motilin gene polymorphisms in children with functional constipation.
Arslan, N; Bozkaya, Ö; Çirali, C; Ercal, D; Küme, T; Ülgenalp, A; Ulusoy, E, 2021
)
1.82
"Motilin is a hormone released by the endocrine cells of the duodenal mucosa during fasting to stimulate gastrointestinal motility. "( Motilin and ghrelin as prokinetic drug targets.
De Smet, B; Depoortere, I; Mitselos, A, 2009
)
3.24
"Motilin is a circulating gastrointestinal peptide secreted primarily by duodenal mucosal M cells and recognized for its prokinetic effects on gastrointestinal tissues. "( Motilin stimulates preadipocyte proliferation and differentiation and adipocyte lipid storage.
Cianflone, K; Miegueu, P; Richard, D; St-Pierre, DH, 2011
)
3.25
"Motilin is a 22-amino-acid gastrointestinal polypeptide that was first isolated from the porcine intestine. "( Anxiolytic actions of motilin in the basolateral amygdala.
Feng, B; Guo, YY; Li, XQ; Liu, JC; Ozaki, K; Yi, DH; Zhang, J; Zhao, MG, 2013
)
2.15
"Motilin is a peptide hormone that regulates gastric motility."( Effects of erythromycin on plasma gastrin, somatostatin, and motilin levels in healthy volunteers and postoperative cancer patients.
Itoh, H; Katagiri, F; Takeyama, M, 2005
)
1.29
"Motilin is a key factor in triggering interdigestive migrating contractions. "( Motilin inhibits ganglionic transmission in the myenteric plexus of the guinea-pig ileum.
Hirai, K; Honda, K; Katayama, Y; Noda, Y, 2005
)
3.21
"Motilin is an important endogenous regulator of gastrointestinal motor function, mediated by the class I G protein-coupled motilin receptor. "( Mutational analysis of predicted intracellular loop domains of human motilin receptor.
Dong, M; Furukawa, S; Hiasa, Y; Matsuura, B; Miller, LJ; Onji, M; Tokunaga, H; Ueda, T, 2008
)
2.02
"Motilin is a hormone produced from endocrine cells of the duodenal mucosa to help regulate motility of the digestive tract. "( Motilin.
Peeters, TL; Poitras, P, 2008
)
3.23
"Motilin is a member of the peptide family that includes ghrelin whose cDNA also encodes a new candidate peptide, obestatin. "( Motilin.
Peeters, TL; Poitras, P, 2008
)
3.23
"Motilin is a fascinating hormone for the physiologist. "( Motilin.
Peeters, TL; Poitras, P, 2008
)
3.23
"Motilin is an intestinal peptide hormone that binds to a membrane bound receptor located in the gut tissue. "( Induction of secondary structure in the peptide hormone motilin by interaction with phospholipid vesicles.
Backlund, BM; Gräslund, A; Peeters, TL; Wikander, G, 1994
)
1.98
"Motilin is a gastrointestinal peptide that stimulates the gastrointestinal motility in several species. "( Effect of motilin on the L-leucine transport in rabbit jejunum.
Alcalde, AI; Marco, R; Navarro, H; Rodriguez-Yoldi, MJ; Sorribas, V, 1995
)
2.14
"Motilin is a 22-residue peptide stimulating stomach and intestinal motility. "( Structural effects of the selective reduction of amide carbonyl groups in motilin 1-12 as determined by nuclear magnetic resonance.
Boulanger, Y; Chen, Y; Gagnon, D; Khiat, A; Poitras, P; St-Pierre, S, 1995
)
1.96
"Motilin is a regulatory polypeptide of 22 amino acid residues and orginates in motilin cells scattered in the duodenal epithelium of most mammals and chickens. "( Motilin and clinical application.
Itoh, Z, 1997
)
3.18
"Motilin is a potent agonist for gastrointestinal smooth muscle contraction and has been proposed to regulate the onset of phase III of the migrating motor complex in dogs and humans. "( Motilin and OHM-11526 activate a calcium current in human and canine jejunal circular smooth muscle.
Farrugia, G; Galdes, A; Macielag, MJ; Peeters, TL; Sarr, MG; Szurszewski, JH, 1997
)
3.18
"Motilin is a 22-amino acid peptide hormone expressed throughout the gastrointestinal (GI) tract of humans and other species. "( Receptor for motilin identified in the human gastrointestinal system.
Abramovitz, M; Austin, CP; Bakshi, R; Cascieri, MA; Evans, J; Feighner, SD; Figueroa, D; Howard, AD; Hreniuk, DL; Kargman, S; MacNeil, D; McKee, KK; Nargund, R; O'Neill, G; Palyha, OC; Patchett, AA; Pong, SS; Smith, RG; Stocco, R; Tan, CP; Van Der Ploeg, LH, 1999
)
2.12
"Motilin is an intestinal peptide that stimulates contraction of gut smooth muscle. "( Motilin receptors in the human antrum.
Dagenais, M; Lapointe, R; Miller, P; Poitras, P; Roy, A; St-Pierre, S, 2000
)
3.19
"Motilin is a hormonal peptide found in the duodenum and jejunum which potently influences gastrointestinal tract motility. "( Release of motilin by oral and intravenous nutrients in man.
Adrian, TE; Besterman, HS; Bloom, SR; Christofides, ND; Ghatei, MA, 1979
)
2.09
"Motilin is a gut hormone, which is involved in gastrointestinal motility. "( Capillary zone electrophoresis studies of motilin peptides. Effects of charge, hydrophobicity, secondary structure and length.
Florance, JR; Galdes, A; Konteatis, ZD; Lessor, RA; Macielag, MJ, 1991
)
1.99
"Motilin is a 22 amino acid polypeptide stimulating intestinal muscle contraction. "( Stimulation of duodenal muscle contraction by porcine or canine motilin in the dog in vivo.
Lahaie, RG; Poitras, P; St-Pierre, S; Trudel, L, 1990
)
1.96
"Motilin is a 22 amino acid peptide first isolated and sequenced from porcine gut. "( Heterogeneity of motilin immunoreactivity in mammalian tissue.
Adelman, JP; Beinfeld, MC; Bond, CT; Daikh, D; Godfrey, B; Nilaver, G, 1988
)
2.06

Effects

Motilin gene has a high homology sequence with that of other mammals, including humans. Motilin has a potent and selective gastric vasodilator effect, which appears to be mediated by both cholinergic and noncholinergic mechanisms.

Motilin has been proposed to initiate the peristaltic reflex in the small intestine and cholecystokinin the gastrocolic reflex. Motilin is implicated in this process, although the exact mechanism is unknown.

ExcerptReferenceRelevance
"The motilin gene has a high homology sequence with that of other mammals, including humans."( House musk shrew (Suncus murinus, order: Insectivora) as a new model animal for motilin study.
Itoh, Z; Kajihara, K; Oda, S; Sakai, T; Sakata, I; Tsutsui, C; Yanaka, T, 2009
)
1.06
"Motilin has a potent and selective gastric vasodilator effect, which appears to be mediated by both cholinergic and noncholinergic mechanisms. "( Motilin regulates interdigestive gastric blood flow in dogs.
Hayakawa, T; Ishiguro, H; Ito, O; Jin, C; Kitagawa, M; Muxin, W; Nakajima, M; Naruse, S; Yokohata, K, 2002
)
3.2
"Motilin has a stimulating effect on gastrointestinal motility. "( Motilin receptors on isolated gastric smooth muscle cells.
Louie, DS; Owyang, C, 1988
)
3.16
"Motilin has been identified in various mammals, but the physiological roles of motilin in regulating GI motility in these mammals are well not understood due to inconsistencies between studies conducted on different species using a range of experimental conditions."( Motilin Comparative Study: Structure, Distribution, Receptors, and Gastrointestinal Motility.
Kaiya, H; Kitazawa, T, 2021
)
2.79
"Motilin has been proposed to initiate the peristaltic reflex in the small intestine and cholecystokinin the gastrocolic reflex."( Disturbed motilin and cholecystokinin release in the irritable bowel syndrome.
Ekman, R; Lindgren, S; Rehfeld, JF; Sjölund, K, 1996
)
1.42
"Motilin has been implicated in this process, although the exact mechanism is unknown."( Motilin: a mechanism incorporating the opossum lower esophageal sphincter into the migrating motor complex.
Blank, E; Dodds, WJ; Holloway, RH; Layman, RD; Takahashi, I, 1985
)
2.43

Actions

Motilin increases lower esophageal sphincter pressure, enhances gastric pepsin secretion and slows down gastric evacuation. The motilin response was lower (P < .03) for encopretic children than for controls. Motilin could increase [Ca+]i.

ExcerptReferenceRelevance
"Mean motilin increase and day 16 mean values were greater for the intervention, compared with the control group (P = .001, P = .005, respectively), while gastrin remained high in both groups. "( Motilin and gastrin secretion and lipid profile in preterm neonates following prebiotics supplementation: a double-blind randomized controlled study.
Boutsikou, T; Briana, DD; Costalos, C; Dasopoulou, M; Karakasidou, E; Malamitsi-Puchner, A; Roma, E, 2015
)
2.37
"Motilin plays an important role in the regulation of interdigestive gastric blood flow in dogs."( Motilin regulates interdigestive gastric blood flow in dogs.
Hayakawa, T; Ishiguro, H; Ito, O; Jin, C; Kitagawa, M; Muxin, W; Nakajima, M; Naruse, S; Yokohata, K, 2002
)
2.48
"Motilin can increase [Ca(2+)]i, and erythromycin also has this effect by binding to motilin receptor."( [Effects of motilin agonists on intracellular calcium mobilization in cultured rat myenteric neurons].
Dong, L; Yang, X; Yang, XE, 2006
)
2.16
"Motilin could increase [Ca+]i."( [Evidence for the presence of motilin receptor and a study on the mechanism of motilin induced Ca2+ signaling in rat myenteric neurons].
Dong, L; Yang, H; Yang, X, 2006
)
1.34
"The motilin response was lower (P < .03) for encopretic children than for controls."( Increased plasma levels of pancreatic polypeptide and decreased plasma levels of motilin in encopretic children.
Fiedorek, SC; Kelleher, K; Mellon, MW; Pope, SK; Rayford, PL; Stern, HP; Stroh, SE, 1995
)
1
"Motilin increases lower esophageal sphincter pressure, enhances gastric pepsin secretion and slows down gastric evacuation."( [New views on gastrointestinal hormones].
Domschke, S; Domschke, W, 1977
)
0.98

Treatment

ExcerptReferenceRelevance
"motilin-treated rats increased in response to exogenous GnRH."( Peripheral or central administration of motilin suppresses LH release in female rats: a novel role for motilin.
Foster, DL; Maekawa, F; Moriyama, R; Niwa, Y; Reyes, BA; Sakai, T; Tsukahara, S; Tsukamura, H, 2000
)
1.3

Toxicity

The outcome parameters included total clinical effectiveness rate (TCE), time for symptom improvement, levels of motilin and corticotropin-releasing hormone (CRH), and adverse events. The secondary outcomes include dyspeptic symptoms, quality of life, mental status, fasting serum gastrin, motil in, and ghrelin concentrations.

ExcerptReferenceRelevance
" The symptoms score, the Nepean Dyspepsia Symptom Index (NDSI), the Nepean Dyspepsia Life Quality Index (NDLQI), Medical Outcomes Study 36-Item Short Form Health Survey (SF-36), electrogastrography, plasma motilin, gastric emptying by B-sonography and adverse reactions were observed before and after treatment, as well as 4 weeks after treatment separately."( [Long-term efficacy and safety research on functional dyspepsia treated with electroacupuncture and Zhizhu Kuanzhong capsule].
Guo, LK; Guo, XF; Zhang, CX, 2011
)
0.56
" No serious adverse reaction was reported in each group."( [Long-term efficacy and safety research on functional dyspepsia treated with electroacupuncture and Zhizhu Kuanzhong capsule].
Guo, LK; Guo, XF; Zhang, CX, 2011
)
0.37
" The secondary outcomes include dyspeptic symptoms, quality of life, mental status, fasting serum gastrin, motilin, and ghrelin concentrations, and adverse events."( Efficacy and safety of manual acupuncture manipulations with different frequencies on epigastric pain syndrome (EPS) in functional dyspepsia (FD) patients: study protocol for a randomized controlled trial.
Bi, Y; Ding, SS; Hong, SH; Wan, YJ; Wu, F; Xu, F; Xuan, LH, 2017
)
0.67
" The outcome parameters included total clinical effectiveness rate (TCE), time for symptom improvement, levels of motilin and corticotropin-releasing hormone (CRH), and adverse events."( Safety and effectiveness of traditional herbal medicine Siho-sogan-san in functional dyspepsia: A systematic review and meta-analysis.
Ha, NY; Jeong, H; Kim, J; Ko, SJ; Lee, H; Park, JW, 2023
)
1.12
"These results suggest that SHS and combination therapy can be considered effective and safe options for the treatment of FD."( Safety and effectiveness of traditional herbal medicine Siho-sogan-san in functional dyspepsia: A systematic review and meta-analysis.
Ha, NY; Jeong, H; Kim, J; Ko, SJ; Lee, H; Park, JW, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
"The study provides pharmacokinetic data for exogenous synthetic and endogenous natural motilin in man."( Pharmacokinetics of motilin in man.
Bloom, SR; Demling, L; Domschke, S; Domschke, W; Mitznegg, P; Wuensch, E, 1977
)
0.8
" To assess its pharmacokinetic parameters in man the MCR and plasma half-life were estimated by the continuous infusion method."( Infusion of a novel peptide, calcitonin gene-related peptide (CGRP) in man. Pharmacokinetics and effects on gastric acid secretion and on gastrointestinal hormones.
Bloom, SR; Ch'ng, JL; Ghatei, MA; Kraenzlin, ME; Mulderry, PK, 1985
)
0.27
" The mean pharmacokinetic parameters were an elimination half-life of 69 h, total systemic clearance of 10 ml/min/kg, and a volume of distribution at steady state of 33."( Safety, toleration, and pharmacokinetics of intravenous azithromycin.
Cohen, SF; Foulds, G; Levy, B; Luke, DR, 1996
)
0.29
"To explore relationship between the essence of Spleen Deficiency Syndrome (SDS) and pharmacokinetic characteristics (PK)."( [Effect of sijunzi decoction on motilin and pharmacokinetic characteristics of tetramethylpyrazine in rat model of spleen deficiency syndrome].
Huang, X; Jiang, YP; Ren, P, 1997
)
0.58
"9 mL/kg), indicating that SK-896 plasma concentrations can be described by a linear pharmacokinetic model within the dose range of the present study."( Pharmacokinetic and pharmacodynamic studies of SK-896, a new human motilin analogue, in healthy male volunteers.
Furuta, Y; Nakashima, M; Nakayama, Y; Suzuki, Y, 2003
)
0.56
" Camicinal was well absorbed, exhibiting linear and approximately dose-proportional pharmacokinetic characteristics and a clear exposure-response relationship with gastric emptying."( The pharmacodynamics, safety and pharmacokinetics of single doses of the motilin agonist, camicinal, in type 1 diabetes mellitus with slow gastric emptying.
Alpers, DH; Barton, ME; Dukes, GE; Hacquoil, K; Hellström, PM; Johnson, LV; Richards, DB; Sanger, GJ; Tack, J, 2016
)
0.67
" Camicinal was well tolerated and exhibited similar pharmacokinetic characteristics in diabetic patients to those previously reported in healthy volunteers."( The pharmacodynamics, safety and pharmacokinetics of single doses of the motilin agonist, camicinal, in type 1 diabetes mellitus with slow gastric emptying.
Alpers, DH; Barton, ME; Dukes, GE; Hacquoil, K; Hellström, PM; Johnson, LV; Richards, DB; Sanger, GJ; Tack, J, 2016
)
0.67

Compound-Compound Interactions

ExcerptReferenceRelevance
"Allantoic endoderm of 3-day chick embryos was combined with pancreatic mesenchyme of 5-day embryos and cultured as chorio-allantoic grafts for a total of 14 days."( Differentiation of endocrine cells in chick allantoic epithelium combined with pancreatic mesenchyme.
Andrew, A; Stein, B, 1989
)
0.28
"To observe the effect of transcutaneous electrical acupoint stimulation (TEAS) combined with general anesthesia on gastric dynamics in controlled hypotension dogs, so as to provide experimental evidence for compound acupuncture anesthesia."( [Effects of transcutaneous electrical acupoint stimulation combined with general anesthesia on changes of gastric dynamics in controlled hypotension dogs].
Dong, ZH; Fang, JQ; Lian, LL; Mo, YD; Shao, XM; Yu, XJ; Zhang, LL, 2011
)
0.37
"Eighteen male beagle dogs were randomly divided into general anesthesia group (GA group, n = 6), general anesthesia + controlled hypotension group (GA + OHT group, n = 6) and general anesthesia combined with TEAS + controlled hypotension group (TEAS group, n = 6)."( [Effects of transcutaneous electrical acupoint stimulation combined with general anesthesia on changes of gastric dynamics in controlled hypotension dogs].
Dong, ZH; Fang, JQ; Lian, LL; Mo, YD; Shao, XM; Yu, XJ; Zhang, LL, 2011
)
0.37
"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."( Effects of intrathecal opioids combined with low-dose naloxone on motilin and its receptor in a rat model of postoperative pain.
Cao, JL; Gao, B; Liu, H; Zhang, Y; Zhao, J; Zheng, B, 2014
)
0.85
" This study was designed to investigate the optimum arecoline content in CAN, using the "target constituent removal combined with bioactivity assay" strategy."( Using the "target constituent removal combined with bioactivity assay" strategy to investigate the optimum arecoline content in charred areca nut.
Gao, YX; Hu, MB; Liu, YJ; Peng, W; Wu, CJ; Yan, D, 2017
)
0.46

Dosage Studied

The biological activity of porcine and canine motilin was studied in rabbits by establishing dose-response curves of both peptides using two different methods. Increasing doses of OHM-11526 shifted the dose- response curves of Motilin and EM-523 to the right, but caused a depression of the maximal response as well. In dogs, Porcine motilIn was inactive at the concentrations tested (up to 10(-4) M) whereas canine motILin induced duodenal contractions in a dose-responsive fashion.

ExcerptRelevanceReference
" Dose-response curves for the LES were constructed from the intravenous bolus injection of graded doses of motilin and gastrin alone and motilin given against a background infusion of secretin."( Effect of motilin on the lower esophageal sphincter of the opossum.
Chey, WY; Gutierrez, JG; Thanik, KD; Yajima, H, 1977
)
0.87
" 13-nle-motilin increased intraluminal pressure in the pylorus and duodenum, and dose-response analysis showed the duodenum to be twice as sensitive as the pylorus to the polypeptide."( Effects of 13-nle-motilin on the electrical and mechanical activity of the isolated perfused canine stomach and duodenum.
Demling, L; Domschke, W; Green, WE; Ritchie, HD; Ruppin, H; Wingate, DL; Wünsch, DE, 1976
)
1.02
" Single injections of neurotensin (1, 2, 4 and 8 micrograms/kg), somatostatin (5, 10 and 20 micrograms/kg) and substance P (1, 2, 4 and 8 micrograms/kg) induced relaxation followed by contraction, but their dose-response relations were obscure."( Effects of gastrointestinal hormones and their related compounds on gastric motility in the rat.
Muto, N; Tani, S, 1985
)
0.27
" Similar dosing without the label was used in motilin, GIP, and insulin studies."( Xylitol vs glucose: effect on the rate of gastric emptying and motilin, insulin, and gastric inhibitory polypeptide release.
Koivistoinen, PE; Kwasowski, P; Marks, V; Porkka, L; Salminen, EK; Salminen, SJ, 1989
)
0.77
" In all cases, BBS and GRP displayed parallel dose-response curves."( Effect of porcine gastrin releasing peptide on gastric secretion and motility and the release of hormonal peptides in conscious cats.
Bernard, C; Chayvialle, JA; Collinet, M; Cuber, JC; McDonald, TJ; Mutt, V; Vagne, M,
)
0.13
" The dose-response effect of synthetic motilin on discharge interval was observed."( [An electromyographic study of the effect of synthetic motilin on gastric motility in dogs].
Murata, S, 1986
)
0.79
"The biological activity of porcine and canine motilin was studied in rabbits by establishing dose-response curves of both peptides using two different methods."( Comparison of the biological activity of canine and porcine motilin in rabbit.
Bormans, V; Matthijs, G; Peeters, TL; Vantrappen, G, 1986
)
0.77
" Dose-response curves to cholecystokinin and acetylcholine were first established."( In vitro effects of pancreatic polypeptide and motilin on contractility of human gallbladder.
Davison, JS; Pomeranz, IS; Shaffer, EA, 1983
)
0.52
" Increasing doses of OHM-11526 shifted the dose-response curves of motilin and EM-523 to the right, but caused a depression of the maximal response as well."( Antagonistic properties of [Phe3,Leu13]porcine motilin.
Depoortere, I; Galdes, A; Macielag, MJ; Peeters, TL, 1995
)
0.78
" Because of the standardized 1-mg/ml infusates, all subjects in the 4-g dosing group complained of an urgent need to urinate."( Safety, toleration, and pharmacokinetics of intravenous azithromycin.
Cohen, SF; Foulds, G; Levy, B; Luke, DR, 1996
)
0.29
"The direct effect of both erythromycin and motilin was a slight increase (less than 10% of the maximal ACh-induced contraction) in the basal tension, with no dose-response relationship."( Effects of erythromycin on human colonic circular muscle in idiopathic chronic constipation.
Altomare, DF; Chieppa, DM; De Salvia, MA; Mansi, G; Mitolo, CI; Montagnani, M; Nacci, C; Potenza, MA; Rinaldi, M; Rinaldi, R; Serio, M, 2000
)
0.57
" A randomized, double-blind, placebo-controlled, three-period incomplete crossover design was used with three dosing periods of 7 days."( The effect of motilin agonist ABT-229 on gastro-oesophageal reflux, oesophageal motility and lower oesophageal sphincter characteristics in GERD patients.
Samsom, M; Smout, AJ; Van Herwaarden, MA; Van Nispen, CH; Verlinden, M, 2000
)
0.67
"To evaluate dose-response effects of motilin and erythromycin on gastric emptying, small bowel and colonic transit in the dog using a validated scintigraphic technique."( Motilides accelerate regional gastrointestinal transit in the dog.
Allen, RG; Chiba, T; Kost, LJ; Phillips, SF; Thomforde, GM, 2000
)
0.58
" After intragastric erythromycin, the authors determined 1) the occurrence and characteristics of phase III of migrating motor complexes, 2) the antral and duodenal motor responses, and 3) the dose-response relation among preterm and full-term infants."( Effect of erythromycin on gastroduodenal contractile activity in developing neonates.
Berseth, CL; Jadcherla, SR, 2002
)
0.31
"To assess non-invasively the dose-response relations for the effects of exogenous motilin on antrum contraction frequency, gall-bladder volume and gastric myoelectrical activity."( Dose-related effects of motilin on proximal gastrointestinal motility.
Biemond, I; Burggraaf, J; Cohen, AF; Jones, R; Kamerling, IM; Masclee, AA; Schoemaker, HC; Van Haarst, AD, 2002
)
0.85
" Thus, we determined the dose-response relationships between enteral feeding volume and gastrointestinal growth and small intestine motor function."( Minimal enteral feeding induces maturation of intestinal motor function but not mucosal growth in neonatal dogs.
Berseth, CL; Burrin, DG; Owens, L, 2002
)
0.31
" Ghrelin was more potent than GHRP-6 and the dose-response relationship for ghrelin but not for GHRP-6 was bell-shaped."( Comparison of the gastroprokinetic effects of ghrelin, GHRP-6 and motilin in rats in vivo and in vitro.
De Man, J; De Winter, B; Depoortere, I; Peeters, T; Pelckmans, P; Thijs, T, 2005
)
0.57
" The rats were divided into six groups after operations at random, which were fed up respectively with Tongjiang granule of different dosage and perpulsid."( [Study on reflux esophagitis treated by Tongjiang granule].
Hu, YC; Shao, Y; Tang, XD; Wang, ZB; Wu, HM, 2006
)
0.33
" In addition, the dosage regimen and target population should be carefully taken into consideration when planning clinical trials."( Potential of ghrelin as a therapeutic approach for gastrointestinal motility disorders.
Peeters, TL, 2006
)
0.33
" Efficacy of medicine in groups with high dosage was stronger than those with low dosage."( [Physiological effects of cold and cool Chinese herbal medicine of channel tropism of stomach on rats with stomach-heat syndrome].
Guo, BJ; Li, XE; Li, XM; Liu, JZ; Sun, GB, 2007
)
0.34
"In a randomized, double-blind design, 106 patients were randomized into four dosing regimens (22 to placebo and 21 each to mitemcinal 10 mg, 20 mg, 30 mg bid or 20 mg tid) for 28 days."( Clinical trial: effect of mitemcinal (a motilin agonist) on gastric emptying in patients with gastroparesis - a randomized, multicentre, placebo-controlled study.
Cynshi, O; McCallum, RW, 2007
)
0.61
"6 g/kg dosage obviously up-regulated 5-HT and DA levels in hippocampus."( Effects of Zuojin pill on depressive behavior and gastrointestinal function in rats with chronic unpredictable mild stress: Role of the brain-gut axis.
Duan, XH; Huang, YZ; Liu, WL; Su, KH; Wang, T; Yan, YF; Yang, L, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Motilin receptorHomo sapiens (human)EC50 (µMol)0.00050.00000.41151.0000AID1889088; AID347506
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (1)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayMotilin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein-coupled peptide receptor activityMotilin receptorHomo sapiens (human)
hormone bindingMotilin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
cytosolMotilin receptorHomo sapiens (human)
plasma membraneMotilin receptorHomo sapiens (human)
plasma membraneMotilin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID1346284Human motilin receptor (Motilin receptor)2006The Journal of biological chemistry, May-05, Volume: 281, Issue:18
Differential contributions of motilin receptor extracellular domains for peptide and non-peptidyl agonist binding and activity.
AID1346284Human motilin receptor (Motilin receptor)2002The Journal of biological chemistry, Mar-22, Volume: 277, Issue:12
Differential determinants for peptide and non-peptidyl ligand binding to the motilin receptor. Critical role of second extracellular loop for peptide binding and action.
AID1346284Human motilin receptor (Motilin receptor)2005The Journal of pharmacology and experimental therapeutics, Jun, Volume: 313, Issue:3
Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog.
AID1346284Human motilin receptor (Motilin receptor)2001The Journal of biological chemistry, Sep-21, Volume: 276, Issue:38
Identification of peptide ligand-binding domains within the human motilin receptor using photoaffinity labeling.
AID1889093Ex vivo agonist activity at GPR38 in rabbit duodenum muscle tissue assessed as intestinal contractile activity2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
AID347512Intrinsic activity at human recombinant motilin receptor expressed in CHO cells relative to motilin2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
AID1889090Agonist activity at rabbit GPR38 expressed in COS-7 cells2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
AID1889088Agonist activity at human GPR38 expressed in COS-7 cells2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
AID347506Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assay2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,296)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990512 (39.51)18.7374
1990's316 (24.38)18.2507
2000's270 (20.83)29.6817
2010's154 (11.88)24.3611
2020's44 (3.40)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 111.69

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index111.69 (24.57)
Research Supply Index7.30 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index206.95 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (111.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials135 (10.10%)5.53%
Reviews0 (0.00%)6.00%
Reviews143 (10.70%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies14 (1.05%)4.05%
Observational0 (0.00%)0.25%
Observational2 (0.15%)0.25%
Other6 (100.00%)84.16%
Other1,043 (78.01%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]