PMID- 10644557
OWN - NLM
STAT- MEDLINE
DCOM- 20000616
LR  - 20181130
IS  - 0193-1857 (Print)
IS  - 0193-1857 (Linking)
VI  - 278
IP  - 1
DP  - 2000 Jan
TI  - Motilin receptors in the human antrum.
PG  - G18-23
AB  - Motilin is an intestinal peptide that stimulates contraction of gut smooth
      muscle. The motilin receptor has not been cloned yet, but motilin-receptor
      agonists appear to be potent prokinetic agents for the treatment of dysmotility
      disorders. The aim of this study was to determine neural or muscular localization
      of motilin receptors in human upper gastrointestinal tract and to investigate
      their pharmacological characteristics. The binding of (125)I-labeled motilin to
      tissue membranes prepared from human stomach and duodenum was studied; rabbit
      tissues were used for comparison. Solutions enriched in neural synaptosomes or in
      smooth muscle plasma membranes were obtained. Various motilin analogs were used
      to displace the motilin radioligand from the various tissue membranes. The
      highest concentration of human motilin receptors was found in the antrum,
      predominantly in the neural preparation. Human motilin receptors were sensitive
      to the NH(2)-terminal portion of the motilin molecule, but comparison with rabbit
      showed that both species had specific affinities for various motilin analogs
      [i.e., Mot-(1-9), Mot-(1-12), Mot-(1-12) (CH(2)NH)(10-11), and erythromycin].
      Motilin receptors obtained from synaptosomes or muscular plasma membranes of
      human antrum expressed different affinity for two motilin-receptor agonists,
      Mot-(1-12) and Mot-(1-12) (CH(2)NH)(10-11), suggesting that they correspond to
      specific receptor subtypes. We conclude that human motilin receptors are located 
      predominantly in nerves of the antral wall, are functionally (and probably
      structurally) different from those found in other species such as the rabbit, and
      express specific functional (and probably structural) characteristics dependent
      on their localization on antral nerves or muscles, suggesting the existence of
      specific receptor subtypes, potentially of significant physiological or
      pharmacological relevance.
FAU - Miller, P
AU  - Miller P
AD  - Gastrointestinal Unit, Centre Hospitalier de l'Universite de Montreal, Montreal, 
      Quebec, Canada H2X 3J4.
FAU - Roy, A
AU  - Roy A
FAU - St-Pierre, S
AU  - St-Pierre S
FAU - Dagenais, M
AU  - Dagenais M
FAU - Lapointe, R
AU  - Lapointe R
FAU - Poitras, P
AU  - Poitras P
LA  - eng
PT  - Journal Article
PL  - United States
TA  - Am J Physiol Gastrointest Liver Physiol
JT  - American journal of physiology. Gastrointestinal and liver physiology
JID - 100901227
RN  - 52906-92-0 (Motilin)
SB  - IM
MH  - Animals
MH  - Humans
MH  - In Vitro Techniques
MH  - Intestinal Mucosa/metabolism
MH  - Motilin/*metabolism
MH  - Muscle, Smooth/metabolism
MH  - Nerve Tissue/metabolism
MH  - Pyloric Antrum/innervation/*metabolism
MH  - Rabbits
MH  - Tissue Distribution
EDAT- 2000/01/25 09:00
MHDA- 2000/06/24 11:00
CRDT- 2000/01/25 09:00
PHST- 2000/01/25 09:00 [pubmed]
PHST- 2000/06/24 11:00 [medline]
PHST- 2000/01/25 09:00 [entrez]
AID - 10.1152/ajpgi.2000.278.1.G18 [doi]
PST - ppublish
SO  - Am J Physiol Gastrointest Liver Physiol. 2000 Jan;278(1):G18-23. doi:
      10.1152/ajpgi.2000.278.1.G18.