In vitro Pharmacological Characterization of Mitemcinal (GM-611), the First Acid-Resistant Non-Peptide Motilin Receptor Agonist, in Smooth Muscle of Rabbit Small Intestine

Pharmacology ◽  
2006 ◽  
Vol 79 (3) ◽  
pp. 137-148 ◽  
Author(s):  
Hisanori Takanashi ◽  
Kenji Yogo ◽  
Ken-ichi Ozaki ◽  
Hiroshi Koga ◽  
Zen Itoh ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Small Intestine ◽  
Receptor Agonist ◽  
Pharmacological Characterization ◽  
Rabbit Small Intestine ◽  
Motilin Receptor

Pharmacological Characterization of a Novel 5-HT4 Receptor Agonist, TS-951, in vitro

Pharmacology ◽  
2001 ◽  
Vol 63 (1) ◽  
pp. 8-16 ◽  
Author(s):  
Sumiyo Kajita ◽  
Chika Ito ◽  
Reiko Kawamura ◽  
Shoji Yasuda ◽  
Yoshihiko Isobe ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Pharmacological Characterization

scholarly journals Pharmacological characterization of a novel 5-HT4 receptor agonist, TS-951 in vitro.

1999 ◽  
Vol 79 ◽  
pp. 206
Author(s):  
Sumiyo Kajita ◽  
Chika Ito ◽  
Yoshihiko Isobe ◽  
Kiyomi Fukushima
Keyword(s):  
Receptor Agonist ◽  
Pharmacological Characterization

1054 PHARMACOLOGICAL CHARACTERIZATION OF HUMAN MALE URETHRAL SMOOTH MUSCLE: AN IN VITRO APPROACH

2010 ◽  
Vol 9 (2) ◽  
pp. 330
Author(s):  
G.T. Kedia ◽  
S. Ückert ◽  
M. Seidler ◽  
J.E. Sonnenberg ◽  
M.A. Kuczyk
Keyword(s):  
Smooth Muscle ◽  
Pharmacological Characterization ◽  
Human Male ◽  
Urethral Smooth Muscle

Morphological and Pharmacological Characterization of Guinea-Pig Prostatic Smooth Muscle Cells in Vitro

1997 ◽  
Vol 4 (2) ◽  
pp. 186-190 ◽  
Author(s):  
Naohito Mikuma ◽  
Seiji Furuya ◽  
Hiroshi Isomura ◽  
Hideo Yabu ◽  
Norimasa Sawada ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Guinea Pig ◽  
Smooth Muscle Cells ◽  
Muscle Cells ◽  
Pharmacological Characterization

Erythromycin is a motilin receptor agonist

1989 ◽  
Vol 257 (3) ◽  
pp. G470-G474 ◽  
Author(s):  
T. Peeters ◽  
G. Matthijs ◽  
I. Depoortere ◽  
T. Cachet ◽  
J. Hoogmartens ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Motor Activity ◽  
Receptor Agonist ◽  
Contractile Response ◽  
Muscle Membrane ◽  
Smooth Muscle Membrane ◽  
Gastrointestinal Motor ◽  
Erythromycin A ◽  
Motilin Receptor

Erythromycin A (EMA) is a potent stimulator of gastrointestinal motor activity. In vitro studies suggest that it mimics motilin, a peptide that stimulates motor activity in human and in rabbit via smooth muscle receptors. We have compared the in vitro contractile effect of EMA and two derivatives, 8,9-anhydro-EMA-6,9-hemiketal (EM201) and EMA N-oxide, on rabbit duodenal smooth-muscle strips with their ability to displace iodinated motilin bound to crude smooth-muscle membrane fractions. The concentrations required to induce 50% of the maximum contractile response to a supramaximal dose of acetylcholine were 5.0 x 10(-8), 2.0 x 10(-6), and 1.0 x 10(-4) M for, respectively, EM201, EMA, and EMA N-oxide. The concentrations required to displace 50% of the labeled motilin were, in the same order, 1.0 x 10(-8), 1.3 x 10(-7), and 4.0 x 10(-6) M. Both parameters were well correlated. The dose-response curve of the EMA was parallel to that of motilin and the effects of motilin and EMA were additive. Contractions induced by EMA were insensitive to pretreatment with tetrodotoxin or atropine. EMA had no effect on muscle strips of rat or dog duodenum but did induce contractions in human strips. EMA was totally ineffective on ileal preparations, which are also unresponsive to motilin and in which motilin binding is absent. EMA has therefore the same regional and species specificity as motilin. We conclude that EMA is a motilin receptor agonist.

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