PMID- 29274880
OWN - NLM
STAT- MEDLINE
DCOM- 20180814
LR  - 20210223
IS  - 1872-6240 (Electronic)
IS  - 0006-8993 (Linking)
VI  - 1680
DP  - 2018 Feb 1
TI  - CB(1) cannabinoid receptor agonist mouse VD-hemopressin(alpha) produced supraspinal 
      analgesic activity in the preclinical models of pain.
PG  - 155-164
LID - S0006-8993(17)30547-4 [pii]
LID - 10.1016/j.brainres.2017.12.013 [doi]
AB  - Mouse VD-hemopressin(alpha) (VD-Hpalpha) is an undecapeptide that selectively activates 
      CB(1) cannabinoid receptor in in vitro functional tests, and exerts 
      CB(1)-mediated central antinociception in the mouse tail-flick assay. The aim of 
      the present study was to further investigate the analgesic properties of 
      supraspinal mouse VD-Hpalpha in a range of preclinical pain models. Our results 
      indicated that the classical cannabinoid agonist WIN 55,212-2 produced 
      supraspinal analgesia in preclinical pain models, which was selectively 
      antagonized by the CB(1) antagonist/inverse agonist AM251, but not by the CB(2) 
      antagonist AM630. In contrast, in post-operative pain model and phase I of 
      formalin test, intracerebroventricular administration of mouse VD-Hpalpha induced 
      dose-related analgesia in mice, which were markedly reduced by pretreatment with 
      the CB(1) neutral antagonist AM4113, but not AM251, AM630 and the selective 
      antagonists of opioid and Transient Receptor Potential Vanilloid Type 1 (TRPV(1)) 
      receptors. Furthermore, in the acetic acid-induced visceral pain model, 
      supraspinal administration of mouse VD-Hpalpha dose-dependently produced analgesic 
      activities and the effects were significantly antagonized by both AM4113 and the 
      TRPV(1) receptor antagonist SB366791, but not AM251, AM630 and naloxone. In 
      addition, central injection of mouse VD-Hpalpha did not have significant effect in 
      phase II of formalin test. Taken together, the present work suggests that the 
      CB(1) receptor peptidic agonist mouse VD-Hpalpha produces supraspinal analgesia in 
      preclinical pain models via a novel CB(1) receptor-mediated mechanism, in a 
      manner pharmacologically dissociable from WIN 55,212-2. In addition, TRPV(1) 
      receptor might also be involved in mouse VD-Hpalpha-induced analgesia in a visceral 
      pain model.
CI  - Copyright (c) 2017 Elsevier B.V. All rights reserved.
FAU - Zheng, Ting
AU  - Zheng T
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China; Department of Clinical Medicine, 
      Gansu Health Vocational College, 60 Donggang West Road, Lanzhou 730000, China.
FAU - Zhang, Run
AU  - Zhang R
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China; Department of Clinical Medicine, 
      Gansu Health Vocational College, 60 Donggang West Road, Lanzhou 730000, China.
FAU - Zhang, Ting
AU  - Zhang T
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China.
FAU - Zhang, Meng-Na
AU  - Zhang MN
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China.
FAU - Xu, Biao
AU  - Xu B
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China.
FAU - Song, Jing-Jing
AU  - Song JJ
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China.
FAU - Li, Ning
AU  - Li N
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China.
FAU - Tang, Hong-Hai
AU  - Tang HH
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China.
FAU - Wang, Pei
AU  - Wang P
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China.
FAU - Wang, Rui
AU  - Wang R
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China. Electronic address: 
      wangrui@lzu.edu.cn.
FAU - Fang, Quan
AU  - Fang Q
AD  - Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and 
      Institute of Physiology, School of Basic Medical Sciences, Lanzhou University, 
      199 Donggang West Road, Lanzhou 730000, China. Electronic address: 
      fangq@lzu.edu.cn.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20171221
PL  - Netherlands
TA  - Brain Res
JT  - Brain research
JID - 0045503
RN  - 0 (Analgesics)
RN  - 0 (Benzoxazines)
RN  - 0 (Cannabinoid Receptor Agonists)
RN  - 0 (Cannabinoid Receptor Antagonists)
RN  - 0 (Morpholines)
RN  - 0 (Naphthalenes)
RN  - 0 (Oligopeptides)
RN  - 0 (VDPVNFKLLSH-OH)
RN  - 1HG84L3525 (Formaldehyde)
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)
RN  - Q40Q9N063P (Acetic Acid)
SB  - IM
MH  - Acetic Acid/toxicity
MH  - Analgesics/*therapeutic use
MH  - Animals
MH  - Benzoxazines/therapeutic use
MH  - Cannabinoid Receptor Agonists/*therapeutic use
MH  - Cannabinoid Receptor Antagonists/therapeutic use
MH  - Disease Models, Animal
MH  - Dose-Response Relationship, Drug
MH  - Formaldehyde/toxicity
MH  - Injections, Spinal
MH  - Male
MH  - Mice
MH  - Morpholines/therapeutic use
MH  - Naphthalenes/therapeutic use
MH  - Oligopeptides/*therapeutic use
MH  - Pain/*drug therapy/etiology
MH  - Pain Measurement
MH  - Rotarod Performance Test
OTO - NOTNLM
OT  - Antinociception
OT  - Cannabinoids
OT  - Formalin pain
OT  - Post-operative pain
OT  - VD-hemopressin(alpha)
OT  - Visceral pain
EDAT- 2017/12/25 06:00
MHDA- 2018/08/15 06:00
CRDT- 2017/12/25 06:00
PHST- 2017/01/04 00:00 [received]
PHST- 2017/10/15 00:00 [revised]
PHST- 2017/12/12 00:00 [accepted]
PHST- 2017/12/25 06:00 [pubmed]
PHST- 2018/08/15 06:00 [medline]
PHST- 2017/12/25 06:00 [entrez]
AID - S0006-8993(17)30547-4 [pii]
AID - 10.1016/j.brainres.2017.12.013 [doi]
PST - ppublish
SO  - Brain Res. 2018 Feb 1;1680:155-164. doi: 10.1016/j.brainres.2017.12.013. Epub 
      2017 Dec 21.