PMID- 7752081
OWN - NLM
STAT- MEDLINE
DCOM- 19950619
LR  - 20191210
IS  - 0022-3565 (Print)
IS  - 0022-3565 (Linking)
VI  - 273
IP  - 2
DP  - 1995 May
TI  - alpha N-acetyl-beta-endorphin-(1-31) disrupts the diminishing effect of 
      mastoparan on opioid- and clonidine-evoked supraspinal antinociception in mice.
PG  - 787-92
AB  - Intracerebroventricular (i.c.v.) administration to mice of the venom 
      tetradecapeptide mastoparan (MP), which binds certain G transducer proteins, 
      resulted in a long-lasting reduction of the supraspinal antinociception induced 
      by opioids and clonidine, the alpha-2 adrenoceptor agonist. The alpha N-acetyl 
      derivative of beta-endorphin-(1-31) (NAC-beta-END; 1 pmol, i.c.v. per mouse) 
      injected 1 hr before an equimolar dose of MP lessened the antagonist activity of 
      the venom peptide on the antinociception induced by D-pen2,5-enkephalin, 
      [D-Ala2]deltorphin II, D-Ala2-N-MePhe4-Gly-ol5-enkephalin and clonidine when 
      evaluated 24 hr later with the tail-flick test. The impairment exerted by MP on 
      these analgesic substances was not altered when NAC-beta-END was administered 
      after the venom peptide. Therefore, the antinociceptive effect depends on which 
      peptide was injected first. The protective activity of NAC-beta-END against MP 
      antagonism of opioid/clonidine antinociception was dose related and exerted at 
      attomolar and femtomolar doses. This finding strengthens the idea of a neural 
      substrate (possibly G proteins) distinct from the opioid receptor enacted by 
      NAC-beta-END to modulate opioid/clonidine antinociception. This research shows 
      that a series of substances, neuropeptides and venoms dissimilarly influence the 
      functional state of G proteins, thus altering the agonist-activated transduction 
      cascade.
FAU - Sanchez-Blazquez, P
AU  - Sanchez-Blazquez P
AD  - Instituto Cajal, C.S.I.C., Madrid, Spain.
FAU - Garzon, J
AU  - Garzon J
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - J Pharmacol Exp Ther
JT  - The Journal of pharmacology and experimental therapeutics
JID - 0376362
RN  - 0 (Analgesics, Opioid)
RN  - 0 (Intercellular Signaling Peptides and Proteins)
RN  - 0 (Peptide Fragments)
RN  - 0 (Peptides)
RN  - 0 (Receptors, Adrenergic, alpha-2)
RN  - 0 (Wasp Venoms)
RN  - 60617-12-1 (beta-Endorphin)
RN  - 72093-21-1 (mastoparan)
RN  - MN3L5RMN02 (Clonidine)
SB  - IM
MH  - Analgesics, Opioid/*pharmacology
MH  - Animals
MH  - Clonidine/*pharmacology
MH  - Intercellular Signaling Peptides and Proteins
MH  - Male
MH  - Mice
MH  - Peptide Fragments/*pharmacology
MH  - Peptides
MH  - Receptors, Adrenergic, alpha-2/drug effects
MH  - Spine
MH  - Wasp Venoms/*antagonists & inhibitors
MH  - beta-Endorphin/*analogs & derivatives
EDAT- 1995/05/01 00:00
MHDA- 1995/05/01 00:01
CRDT- 1995/05/01 00:00
PHST- 1995/05/01 00:00 [pubmed]
PHST- 1995/05/01 00:01 [medline]
PHST- 1995/05/01 00:00 [entrez]
PST - ppublish
SO  - J Pharmacol Exp Ther. 1995 May;273(2):787-92.