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Chemical Compound Review

AC1MHYOD     (2S)-2-[[(2S)-2-[2-[2-[[(2S)- 2-(diprop-2...

Synonyms: SureCN4405821, ICI-154129, DCL000416, DNC000771, LS-177751, ...
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Disease relevance of ICI-154129


Psychiatry related information on ICI-154129

  • The drug ICI 154129 (30 mg/kg, s.c.) failed to prevent the antinociceptive effects and stimulation of locomotor activity produced by etorphine, whereas the relatively selective mu-opioid receptor antagonist, naloxone was effective in both test situations [2].
  • Naloxone (mu selective) and MR2266 BS (kappa selective) potentiated the OT response to an emotional stress (1 min. immobilization) whereas the delta selective antagonist ICI 154129 was without effect [3].

High impact information on ICI-154129

  • The delta-antagonist ICI 154129 never affected PRL or LH concentrations, whereas both the mu- and kappa-antagonists, naloxone and MR 1452, respectively, seemed to be effective [4].
  • Selective kappa (binaltorphimine) and delta (ICI 154129 and ICI 174864) antagonists were used to see whether these other receptors might be involved in mediating morphine analgesia in beta-FNA-treated animals [5].
  • Comparison in the mouse of the effect of the opiate delta receptor antagonist ICI 154129 and naloxone in tests of extinction, passive avoidance and food intake [6].
  • We used rats to study the ability of a selective opioid delta receptor antagonist (ICI 154129) to prevent the effect of ethanol on pain sensitivity, body temperature, sensorimotor performance and level of consciousness [7].
  • The stimulatory actions of morphine and Tyr-D-Ala-Gly-MePhe-NH(CH2)2OH on CRF release were antagonized by naloxone (10(-8) M) and by the mu/delta-opioid receptor antagonist, beta-funaltrexamine (beta-FNA, 10(-9) M), but not by the delta-opioid receptor antagonist, ICI-154129 (5 X 10(-6) M) [8].

Biological context of ICI-154129

  • A long term treatment with the delta-selective opiate antagonist NN-bisallyl-Tyr-Gly-Gly-psi-(CH2S)-Phe-Leu-OH (ICI 154129) produces an increase in the number of delta-opiate binding sites, whereas the same treatment with the non selective opiate antagonist naloxone results in an enhancement of both mu- and delta-binding sites [9].

Anatomical context of ICI-154129

  • The Ke values of three antagonists, naloxone, Mr 2266 and ICI 154129, against dynorphin-(1-8) in the presence of the three peptidase inhibitors indicated that dynorphin-(1-8) acted on kappa receptors in guinea-pig ileum and on both kappa and delta receptors in mouse vas deferens [10].

Gene context of ICI-154129


Analytical, diagnostic and therapeutic context of ICI-154129

  • The mu antagonist beta-funaltrexamine, at doses that antagonized morphine analgesia, failed to alter shock, whereas the delta antagonist M 154,129: [N,N-bisallyl-Tyr-Gly-Gly-psi-(CH2S)-Phe-Leu-OH] (ICI) reversed shock at doses that failed to block morphine analgesia [12].
  • However, the injection of 10 mg/kg ICI-154129 prevented hyperthermia-induced convulsions (only 20% of the rats showed generalized convulsions at 90 min) [13].


  1. M 154,129, a putative delta antagonist, reverses endotoxic shock without altering morphine analgesia. Holaday, J.W., Ruvio, B.A., Robles, L.E., Johnson, C.E., D'Amato, R.J. Life Sci. (1982) [Pubmed]
  2. In vivo evidence for the selectivity of ICI 154129 for the delta-opioid receptor. Priestley, T., Turnbull, M.J., Wei, E. Neuropharmacology (1985) [Pubmed]
  3. Opioid control of oxytocin secretion: evidence of distinct regulatory actions of two opiate receptor types. Carter, D.A., Lightman, S.L. Life Sci. (1987) [Pubmed]
  4. Mainly mu-opiate receptors are involved in luteinizing hormone and prolactin secretion. Panerai, A.E., Petraglia, F., Sacerdote, P., Genazzani, A.R. Endocrinology (1985) [Pubmed]
  5. Evidence for the interaction of morphine with kappa and delta opioid receptors to induce analgesia in beta-funaltrexamine-treated mice. Takemori, A.E., Portoghese, P.S. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  6. Comparison in the mouse of the effect of the opiate delta receptor antagonist ICI 154129 and naloxone in tests of extinction, passive avoidance and food intake. Benton, D., Dalrymple-Alford, J.C., McAllister, K.H., Brain, P.F., Brain, S. Psychopharmacology (Berl.) (1984) [Pubmed]
  7. Evidence from behavioural and in vitro receptor binding studies that the enkephalinergic system does not mediate acute ethanol effects. Jørgensen, H.A., Hole, K. Eur. J. Pharmacol. (1986) [Pubmed]
  8. Pharmacological characterization of opioid receptors influencing the secretion of corticotrophin releasing factor in the rat. Buckingham, J.C., Cooper, T.A. Neuroendocrinology (1986) [Pubmed]
  9. Behavioural and biochemical effects in C57BL/6J mice after a prolonged treatment with the delta-opiate antagonist ICI 154129. Volterra, A., Brunello, N., Cagiano, R., Cuomo, V., Racagni, G. J. Pharm. Pharmacol. (1984) [Pubmed]
  10. Inactivation of dynorphin-(1-8) in isolated preparations by three peptidases. Numata, H., Hiranuma, T., Oka, T. Jpn. J. Pharmacol. (1988) [Pubmed]
  11. Effects of opioid agonists and antagonists on oxytocin and vasopressin release in vitro. Bicknell, R.J., Chapman, C., Leng, G. Neuroendocrinology (1985) [Pubmed]
  12. Multiple opioid receptors in endotoxic shock: evidence for delta involvement and mu-delta interactions in vivo. D'Amato, R., Holaday, J.W. Proc. Natl. Acad. Sci. U.S.A. (1984) [Pubmed]
  13. Prevention of hyperthermia-induced convulsions in immature rat by MR-2266, a kappa antagonist. Laorden, M.L., Carrillo, E., Puig, M.M. Methods and findings in experimental and clinical pharmacology. (1991) [Pubmed]
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