| In vitro characterization of the effects of endomorphin 1 and 2, endogenous ligands for mu-opioid receptors, on mouse colonic motility. | |
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MedLine Citation:
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PMID: 17274956 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The effects of endomorphin 1 (EM1) and 2 (EM2) in colonic motility remain unknown. We investigated the effects and mechanisms of these endomorphins (EMs) on the colonic motility in vitro by applying various neural blocking agents and various opioid receptor antagonists. EMs (10(-9) to 10(-6)M) displayed significant stimulatory effects on the basal tonus or spontaneous activity of mouse colon but not of stomach and small intestine. It is noteworthy that the contractile actions of EMs varied slightly among different regions of colonic longitudinal muscle layers, whereas the contractile responses induced by EMs were significantly different among different regions of circular muscle layers. EMs-induced longitudinal or circular muscle contractions were not significantly affected by atropine, N(G)-nitro-l-arginine methyl ester, phentolamine, propranolol and methysergide. Tetrodotoxin, indomethacin and naloxone completely abolished the EMs-induced colonic contractions. Surprisingly, EMs (10(-7)M)-induced longitudinal muscle contractions were significantly attenuated by nor-binaltorphimine (3x10(-6)M). By contrast, pretreatment with naltrindole (10(-6)M) did not significantly affect EMs-induced longitudinal or circular muscle contractions. Interestingly, the circular muscle contractions in response to EM2 (10(-7)M) were not fully blocked by beta-funaltrexamine (6x10(-6)M). Naloxonazine (10(-6)M) almost fully antagonized the EMs-induced longitudinal or circular muscle contractions, and these effects could be only partially reversed by extensive washing. All the results indicated that the mechanisms and sites of actions of EMs were region-specific. Furthermore, these findings showed that the activation of multiple subtypes of opioid receptors, possibly including mu(1) (naloxonazine-sensitive), mu(2) and even other forms of muORs (beta-FNA-insensitive), was required for EMs-induced mouse colonic motility. |
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Authors:
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Ye Yu; Yun Cui; Xiang Wang; Lu-hao Lai; Chang-Lin Wang; Ying-zhe Fan; Jing Liu; Rui Wang |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2007-01-10 |
Journal Detail:
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Title: Biochemical pharmacology Volume: 73 ISSN: 0006-2952 ISO Abbreviation: Biochem. Pharmacol. Publication Date: 2007 May |
Date Detail:
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Created Date: 2007-03-27 Completed Date: 2007-05-17 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0101032 Medline TA: Biochem Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 1384-93 Citation Subset: IM |
Affiliation:
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Institute of Biochemistry and Molecular Biology, State Key Laboratory of Applied Organic Chemistry, Lanzhou University, 222 Tian Shui South Road, Lanzhou 730000, China. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Analgesics, Opioid
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pharmacology Animals Colon / cytology Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / pharmacology Gastrointestinal Motility / drug effects* Intestine, Small / cytology Mice Morphine / pharmacology Muscle Contraction / drug effects Muscle, Smooth / drug effects*, physiology Oligopeptides / pharmacology* Receptors, Opioid, mu / drug effects, physiology* Stomach / cytology |
| Chemical | |
Reg. No./Substance:
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0/Analgesics, Opioid; 0/Oligopeptides; 0/Receptors, Opioid, mu; 0/endomorphin 1; 100929-53-1/Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; 57-27-2/Morphine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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