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Pharmacological effects of the dansylated neuropeptide FF analogues on body temperature and morphine analgesia.
Neuropeptides. 2007 Oct; 41(5):339-47.N

Abstract

In our previous work, the two putative agonists (dansyl-GSRFamide and dansyl-PQRFamide) and the two putative antagonists (dansyl-GSRamide and dansyl-PQRamide) on neuropeptide FF (NPFF) receptors were synthesized to evaluate the importance of Phe(8) of NPFF. In the present study, these putative NPFF agonists/antagonists containing different N-terminal sequences were further examined for their pharmacological profiles in thermoregulatory and nociceptive tests. The results indicated that the two dansylated agonists potently possessed similar thermoregulation (rank order of potencies: dansyl-GSRFamide>>NPFF>dansyl-PQRFamide) and different modulation of opioid-induced analgesia; in contrast, both of the two putative antagonists exhibited marked hypothermia (rank order of potencies: dansyl-PQRamide>dansyl-GSRamide) and facilitation of morphine analgesia (rank order of potencies: dansyl-PQRamide > dansyl-GSRamide). These data reveal that the difference of the N-terminal residues of the two putative agonists causes their dissociation of pharmacological pro- and anti-opioid effects. In addition, their N-terminal part is important to determine the potency of the dansylated agonists/antagonists. Our work might be helpful to develop a highly potent and fluorescent NPFF ligand.

Authors+Show Affiliations

Key Laboratory of Preclinical Study for New Drugs of Gansu Province, and State Key Laboratory of Applied Organic Chemistry, and Institute of Biochemistry and Molecular Biology, Lanzhou University, 222 Tian Shui South Road, Lanzhou 730000, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

17597204

Citation

Fang, Quan, et al. "Pharmacological Effects of the Dansylated Neuropeptide FF Analogues On Body Temperature and Morphine Analgesia." Neuropeptides, vol. 41, no. 5, 2007, pp. 339-47.
Fang Q, He F, Wang YQ, et al. Pharmacological effects of the dansylated neuropeptide FF analogues on body temperature and morphine analgesia. Neuropeptides. 2007;41(5):339-47.
Fang, Q., He, F., Wang, Y. Q., Guo, J., Zhang, B. Z., Chen, Q., & Wang, R. (2007). Pharmacological effects of the dansylated neuropeptide FF analogues on body temperature and morphine analgesia. Neuropeptides, 41(5), 339-47.
Fang Q, et al. Pharmacological Effects of the Dansylated Neuropeptide FF Analogues On Body Temperature and Morphine Analgesia. Neuropeptides. 2007;41(5):339-47. PubMed PMID: 17597204.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacological effects of the dansylated neuropeptide FF analogues on body temperature and morphine analgesia. AU - Fang,Quan, AU - He,Feng, AU - Wang,Yi-Qing, AU - Guo,Jia, AU - Zhang,Bang-zhi, AU - Chen,Qiang, AU - Wang,Rui, Y1 - 2007/06/26/ PY - 2007/01/19/received PY - 2007/03/28/revised PY - 2007/04/07/accepted PY - 2007/6/29/pubmed PY - 2007/11/14/medline PY - 2007/6/29/entrez SP - 339 EP - 47 JF - Neuropeptides JO - Neuropeptides VL - 41 IS - 5 N2 - In our previous work, the two putative agonists (dansyl-GSRFamide and dansyl-PQRFamide) and the two putative antagonists (dansyl-GSRamide and dansyl-PQRamide) on neuropeptide FF (NPFF) receptors were synthesized to evaluate the importance of Phe(8) of NPFF. In the present study, these putative NPFF agonists/antagonists containing different N-terminal sequences were further examined for their pharmacological profiles in thermoregulatory and nociceptive tests. The results indicated that the two dansylated agonists potently possessed similar thermoregulation (rank order of potencies: dansyl-GSRFamide>>NPFF>dansyl-PQRFamide) and different modulation of opioid-induced analgesia; in contrast, both of the two putative antagonists exhibited marked hypothermia (rank order of potencies: dansyl-PQRamide>dansyl-GSRamide) and facilitation of morphine analgesia (rank order of potencies: dansyl-PQRamide > dansyl-GSRamide). These data reveal that the difference of the N-terminal residues of the two putative agonists causes their dissociation of pharmacological pro- and anti-opioid effects. In addition, their N-terminal part is important to determine the potency of the dansylated agonists/antagonists. Our work might be helpful to develop a highly potent and fluorescent NPFF ligand. SN - 0143-4179 UR - https://www.unboundmedicine.com/medline/citation/17597204/Pharmacological_effects_of_the_dansylated_neuropeptide_FF_analogues_on_body_temperature_and_morphine_analgesia_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0143-4179(07)00038-8 DB - PRIME DP - Unbound Medicine ER -