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Comparison of pharmacological activities of Neuropeptide FF1 and Neuropeptide FF2 receptor agonists.
Eur J Pharmacol. 2005 Jan 31; 508(1-3):107-14.EJ

Abstract

The pharmacological effects of Neuropeptide FF (NPFF) analogs exhibiting different selectivities towards Neuropeptide FF1 (NPFF1) and Neuropeptide FF2 (NPFF2) receptors were investigated after supraspinal administration in mice. Injected into the third ventricle, VPNLPQRF-NH2, which is selective for Neuropeptide FF1 receptor induced a hypothermia while EFWSLAAPQRF-NH2 and SPAFLFQPQRF-NH2 which are selective for Neuropeptide FF2 receptor, did not. Furthermore, EFWSLAAPQRF-NH2 significantly increased the body temperature when compared to saline treated mice, indicating that Neuropeptide FF1 receptor could be responsible for hypothermia while Neuropeptide FF2 mediated an hyperthermic effect. After administration into the lateral ventricle, 1DMe ([D.Tyr1,(N.Me)Phe3]NPFF), a weakly selective Neuropeptide FF2 receptor agonist, exerted a clear anti-opioid effect in the tail flick test. The selective Neuropeptide FF1 receptor agonist VPNLPQRF-NH2 did not induce significant anti-opioid actions but rather increased, dose-dependently, morphine analgesia while EFWSLAAPQRF-NH2, the highest selective Neuropeptide FF2 receptor analog, induced the same pharmacological effect as VPNLPQRF-NH2 at comparable doses. These features indicate that the pro- and anti-opioid actions are not strictly related to the selectivity towards Neuropeptide FF2 or Neuropeptide FF1 receptor. Our data demonstrate that Neuropeptide FF1 and Neuropeptide FF2 receptors differently modulate nervous system functions.

Authors+Show Affiliations

Institut de Pharmacologie et de Biologie Structurale, CNRS UMR 5089, 205 route de Narbonne, 31077 Toulouse Cedex, France.No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15680260

Citation

Quelven, Isabelle, et al. "Comparison of Pharmacological Activities of Neuropeptide FF1 and Neuropeptide FF2 Receptor Agonists." European Journal of Pharmacology, vol. 508, no. 1-3, 2005, pp. 107-14.
Quelven I, Roussin A, Zajac JM. Comparison of pharmacological activities of Neuropeptide FF1 and Neuropeptide FF2 receptor agonists. Eur J Pharmacol. 2005;508(1-3):107-14.
Quelven, I., Roussin, A., & Zajac, J. M. (2005). Comparison of pharmacological activities of Neuropeptide FF1 and Neuropeptide FF2 receptor agonists. European Journal of Pharmacology, 508(1-3), 107-14.
Quelven I, Roussin A, Zajac JM. Comparison of Pharmacological Activities of Neuropeptide FF1 and Neuropeptide FF2 Receptor Agonists. Eur J Pharmacol. 2005 Jan 31;508(1-3):107-14. PubMed PMID: 15680260.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparison of pharmacological activities of Neuropeptide FF1 and Neuropeptide FF2 receptor agonists. AU - Quelven,Isabelle, AU - Roussin,Anne, AU - Zajac,Jean-marie, Y1 - 2005/01/07/ PY - 2004/08/04/received PY - 2004/11/30/revised PY - 2004/12/06/accepted PY - 2005/2/1/pubmed PY - 2005/7/15/medline PY - 2005/2/1/entrez SP - 107 EP - 14 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 508 IS - 1-3 N2 - The pharmacological effects of Neuropeptide FF (NPFF) analogs exhibiting different selectivities towards Neuropeptide FF1 (NPFF1) and Neuropeptide FF2 (NPFF2) receptors were investigated after supraspinal administration in mice. Injected into the third ventricle, VPNLPQRF-NH2, which is selective for Neuropeptide FF1 receptor induced a hypothermia while EFWSLAAPQRF-NH2 and SPAFLFQPQRF-NH2 which are selective for Neuropeptide FF2 receptor, did not. Furthermore, EFWSLAAPQRF-NH2 significantly increased the body temperature when compared to saline treated mice, indicating that Neuropeptide FF1 receptor could be responsible for hypothermia while Neuropeptide FF2 mediated an hyperthermic effect. After administration into the lateral ventricle, 1DMe ([D.Tyr1,(N.Me)Phe3]NPFF), a weakly selective Neuropeptide FF2 receptor agonist, exerted a clear anti-opioid effect in the tail flick test. The selective Neuropeptide FF1 receptor agonist VPNLPQRF-NH2 did not induce significant anti-opioid actions but rather increased, dose-dependently, morphine analgesia while EFWSLAAPQRF-NH2, the highest selective Neuropeptide FF2 receptor analog, induced the same pharmacological effect as VPNLPQRF-NH2 at comparable doses. These features indicate that the pro- and anti-opioid actions are not strictly related to the selectivity towards Neuropeptide FF2 or Neuropeptide FF1 receptor. Our data demonstrate that Neuropeptide FF1 and Neuropeptide FF2 receptors differently modulate nervous system functions. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/15680260/Comparison_of_pharmacological_activities_of_Neuropeptide_FF1_and_Neuropeptide_FF2_receptor_agonists_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(04)01400-1 DB - PRIME DP - Unbound Medicine ER -