PMID- 7925596 OWN - NLM STAT- MEDLINE DCOM- 19941021 LR - 20191210 IS - 0014-2999 (Print) IS - 0014-2999 (Linking) VI - 258 IP - 1-2 DP - 1994 Jun 2 TI - Mastoparan reduces the supraspinal analgesia mediated by mu/delta-opioid receptors in mice. PG - 159-62 AB - Intracerebroventricular (i.c.v.) administration of the venom peptide, mastoparan, to mice decreased to a limited extent opioid-induced supraspinal analgesia in a non-competitive fashion. The mu-opioid receptor agonists, [D-Ala2,N-MePhe4,Gly-ol5]-enkephalin (DAMGO) and morphine, the mu/delta-opioid receptor ligands, human beta-endorphin-(1-31) and [D-Ala2,D-Leu5]-enkephalin (DADLE), and the selective ligands of delta-opioid receptors, [D-Pen2,5]enkephalin (DPDPE) and [D-Ala2]deltorphin II, showed an impaired analgesic effect in mice given mastoparan. Mastoparan diminished the analgesic activity of DPDPE and [D-Ala2]deltorphin II to the same extent as observed after giving the delta-opioid receptor-selective antagonist, ICI 174864. The mu-opioid receptor-mediated analgesia that remained after mastoparan was abolished in the presence of the opioid antagonist, naloxone. Mastoparan after binding to Gi alpha/Go alpha subunits could block opioid antinociception. The existence of a class of G protein functionally coupled to mu-opioid receptors, but resistant to the effect of mastoparan is suggested. FAU - Sanchez-Blazquez, P AU - Sanchez-Blazquez P AD - Instituto Cajal, CSIC, Madrid, Spain. FAU - Garzon, J AU - Garzon J LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Netherlands TA - Eur J Pharmacol JT - European journal of pharmacology JID - 1254354 RN - 0 (Analgesics) RN - 0 (Enkephalins) RN - 0 (Intercellular Signaling Peptides and Proteins) RN - 0 (Peptides) RN - 0 (Receptors, Opioid) RN - 0 (Wasp Venoms) RN - 100929-53-1 (Enkephalin, Ala(2)-MePhe(4)-Gly(5)-) RN - 63631-40-3 (Enkephalin, Leucine-2-Alanine) RN - 72093-21-1 (mastoparan) RN - 88373-73-3 (Enkephalin, D-Penicillamine (2,5)-) RN - EC 3.6.1.- (GTP-Binding Proteins) SB - IM MH - Amino Acid Sequence MH - Analgesics/*antagonists & inhibitors/pharmacology MH - Animals MH - Dose-Response Relationship, Drug MH - Enkephalin, Ala(2)-MePhe(4)-Gly(5)- MH - Enkephalin, D-Penicillamine (2,5)- MH - Enkephalin, Leucine-2-Alanine/pharmacology MH - Enkephalins/pharmacology MH - GTP-Binding Proteins/metabolism MH - Injections, Intraventricular MH - Intercellular Signaling Peptides and Proteins MH - Male MH - Mice MH - Molecular Sequence Data MH - Peptides MH - Receptors, Opioid/*drug effects/metabolism MH - Wasp Venoms/administration & dosage/*pharmacology EDAT- 1994/06/02 00:00 MHDA- 1994/06/02 00:01 CRDT- 1994/06/02 00:00 PHST- 1994/06/02 00:00 [pubmed] PHST- 1994/06/02 00:01 [medline] PHST- 1994/06/02 00:00 [entrez] AID - 0014-2999(94)90070-1 [pii] AID - 10.1016/0014-2999(94)90070-1 [doi] PST - ppublish SO - Eur J Pharmacol. 1994 Jun 2;258(1-2):159-62. doi: 10.1016/0014-2999(94)90070-1.