PMID- 26991932
OWN - NLM
STAT- MEDLINE
DCOM- 20180205
LR  - 20210223
IS  - 1365-2982 (Electronic)
IS  - 1350-1925 (Linking)
VI  - 28
IP  - 6
DP  - 2016 Jun
TI  - Central administrations of hemopressin and related peptides inhibit 
      gastrointestinal motility in mice.
PG  - 891-9
LID - 10.1111/nmo.12789 [doi]
AB  - BACKGROUND: Hemopressin was identified as an endogenous inverse 
      agonist/antagonist of CB1 receptor, whereas VD-hemopressin(alpha) [VD-Hpalpha] and 
      VD-hemopressin(beta) [VD-Hpbeta] were found as the novel endogenous peptidic agonists 
      of cannabinoid receptors. As cannabinoids are potent modulators of 
      gastrointestinal (GI) motility, our aim was to characterize the effects of 
      hemopressin and related peptides on GI motility in vivo. METHODS: The responses 
      of intracerebroventricular (i.c.v.) administration of the reference compound 
      WIN55,212-2, hemopressin, and related peptides to GI motility were investigated 
      by measuring upper GI transit, colonic bead expulsion, and whole gut transit in 
      mice. KEY RESULTS: Central administration of the classical cannabinoid receptor 
      agonist WIN55,212-2 dose-dependently slowed upper GI transit, colonic expulsion, 
      and whole gut transit via CB1 receptor. Similarly, Hpalpha, VD-Hpalpha, and VD-Hpbeta 
      delayed upper GI transit and colonic expulsion after i.c.v. administration. At 
      the high doses, Hpalpha and VD-Hpbeta inhibited whole gut transit, whereas VD-Hpalpha had no 
      effect on whole gut transit. In addition, the effects of these three peptides on 
      GI transit were antagonized by the CB1 receptor selective antagonist AM251, but 
      not by the CB2 receptor selective antagonist AM630. CONCLUSION & INFERENCES: The 
      endogenous cannabinoid peptide ligands hemopressin, VD-Hpalpha, and VD-Hpbeta inhibited 
      GI transit through the activation of CB1 , but not CB2 cannabinoid receptors. The 
      lower potencies of the hemopressin and related peptides in GI transit assays may 
      be important for the future development of cannabinoid peptides as the 
      therapeutic analgesics with limited GI side effects.
CI  - (c) 2016 John Wiley & Sons Ltd.
FAU - Li, X-H
AU  - Li XH
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Lin, M-L
AU  - Lin ML
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Wang, Z-L
AU  - Wang ZL
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Wang, P
AU  - Wang P
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Tang, H-H
AU  - Tang HH
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Lin, Y-Y
AU  - Lin YY
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Li, N
AU  - Li N
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Fang, Q
AU  - Fang Q
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
FAU - Wang, R
AU  - Wang R
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of 
      Physiology, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.
LA  - eng
PT  - Journal Article
DEP - 20160314
PL  - England
TA  - Neurogastroenterol Motil
JT  - Neurogastroenterology and motility
JID - 9432572
RN  - 0 (Analgesics)
RN  - 0 (Benzoxazines)
RN  - 0 (Cannabinoids)
RN  - 0 (Hemoglobins)
RN  - 0 (Morpholines)
RN  - 0 (Naphthalenes)
RN  - 0 (Peptide Fragments)
RN  - 0 (Receptor, Cannabinoid, CB1)
RN  - 0 (hemopressin)
RN  - 5H31GI9502 
      ((3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone)
SB  - IM
MH  - Analgesics/administration & dosage
MH  - Animals
MH  - Benzoxazines/*administration & dosage
MH  - Cannabinoids/*administration & dosage
MH  - Dose-Response Relationship, Drug
MH  - Gastrointestinal Motility/*drug effects/physiology
MH  - Hemoglobins/*administration & dosage
MH  - Injections, Intraventricular
MH  - Male
MH  - Mice
MH  - Morpholines/*administration & dosage
MH  - Naphthalenes/*administration & dosage
MH  - Peptide Fragments/*administration & dosage
MH  - Receptor, Cannabinoid, CB1/agonists/physiology
OTO - NOTNLM
OT  - cannabinoid
OT  - cannabinoid receptor type 1
OT  - colonic bead expulsion gastrointestinal transit
OT  - hemopressin
EDAT- 2016/03/19 06:00
MHDA- 2018/02/06 06:00
CRDT- 2016/03/19 06:00
PHST- 2015/10/10 00:00 [received]
PHST- 2016/01/06 00:00 [accepted]
PHST- 2016/03/19 06:00 [entrez]
PHST- 2016/03/19 06:00 [pubmed]
PHST- 2018/02/06 06:00 [medline]
AID - 10.1111/nmo.12789 [doi]
PST - ppublish
SO  - Neurogastroenterol Motil. 2016 Jun;28(6):891-9. doi: 10.1111/nmo.12789. Epub 2016 
      Mar 14.