PMID- 2901358 OWN - NLM STAT- MEDLINE DCOM- 19881018 LR - 20190624 IS - 0014-2999 (Print) IS - 0014-2999 (Linking) VI - 150 IP - 3 DP - 1988 Jun 10 TI - Central effects of the potent and highly selective mu opioid antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) in mice. PG - 355-60 AB - The ability of the selective cyclic mu-opioid receptor antagonist, D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP), to inhibit the acute and chronic effects of morphine in vivo was studied in mice. Intracerebroventricular (i.c.v.) administration of CTOP antagonized the analgesic effect of morphine in a dose-dependent manner, as measured by the heat-irradiant (tail-flick) method. CTOP was more effective than naloxone in inhibiting analgesia on a molar basis. CTOP also antagonized the acute morphine-induced hypermotility. CTOP caused withdrawal hypothermia and a loss of body weight in morphine-dependent animals. After the development of morphine-induced chronic dependence, CTOP administered i.c.v. caused a dose-dependent loss of body weight and hypothermia, and was about 10-400 times more potent than naloxone. CTOP administered alone to drugnaive mice did not cause antinociception, changes in body weight or body temperature. FAU - Gulya, K AU - Gulya K AD - Central Research Laboratory, Medical University, Szeged, Hungary. FAU - Krivan, M AU - Krivan M FAU - Nyolczas, N AU - Nyolczas N FAU - Sarnyai, Z AU - Sarnyai Z FAU - Kovacs, G L AU - Kovacs GL LA - eng PT - Journal Article PL - Netherlands TA - Eur J Pharmacol JT - European journal of pharmacology JID - 1254354 RN - 0 (Receptors, Opioid) RN - 0 (Receptors, Opioid, mu) RN - 103429-31-8 (phenylalanyl-cyclo(cysteinyltyrosyl-tryptophyl-ornithyl-threonyl-penicillamine)threoninamide) RN - 51110-01-1 (Somatostatin) RN - 76I7G6D29C (Morphine) SB - IM MH - Animals MH - Body Temperature/drug effects MH - Body Weight/drug effects MH - Brain/*drug effects/physiology MH - Drug Tolerance MH - Injections, Intraventricular MH - Male MH - Mice MH - Mice, Inbred Strains MH - Morphine/pharmacology MH - Morphine Dependence/psychology MH - Motor Activity/drug effects MH - Nociceptors/drug effects MH - Pain/physiopathology MH - Reaction Time/drug effects MH - Receptors, Opioid/*metabolism MH - Receptors, Opioid, mu MH - Sensory Thresholds/drug effects MH - Somatostatin/*analogs & derivatives/pharmacology EDAT- 1988/06/10 00:00 MHDA- 1988/06/10 00:01 CRDT- 1988/06/10 00:00 PHST- 1988/06/10 00:00 [pubmed] PHST- 1988/06/10 00:01 [medline] PHST- 1988/06/10 00:00 [entrez] AID - 0014-2999(88)90018-0 [pii] AID - 10.1016/0014-2999(88)90018-0 [doi] PST - ppublish SO - Eur J Pharmacol. 1988 Jun 10;150(3):355-60. doi: 10.1016/0014-2999(88)90018-0.