A comparison of the antinociceptive and temperature responses to morphine and fentanyl derivatives in rats
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2013
Authors
Vujovic, Katarina R. SavicVuckovic, Sonja
Srebro, Dragana
Ivanović, Milovan
Došen-Mićović, Ljiljana
Vucetic, Cedomir
Dzoljic, Eleonora
Prostran, Milica
Article (Published version)
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In addition to producing antinociception, opioids exert profound effects on body temperature. This study aimed at comparing antinociceptive and hyperthermic responses between two groups of mu-opioid receptor agonists: fentanyl (4-anilinopiperidine-type) and morphine (phenanthrene-type) derivatives in rats. Analgesic activity was assessed by tail immersion test and the body temperature by insertion of a thermometer probe into the colon. Fentanyl (F), (+/-)-cis-3-methyl fentanyl (CM), (+/-)-cis-3-carbomethoxy fentanyl (C), (+/-)trans-3-carbomethoxy fentanyl (T) and (+/-)-cis-3 butyl fentanyl (B) produced dose-dependent increase in antinociception and hyperthermia. The relative order of analgesic potency was: CM(11.27) gt F(1) gt C(0.35)a parts per thousand yenT(0.11)a parts per thousand yenB(0.056). Similar to this, the relative order of hyperthermic potency was: CM(8.43) gt F(1) gt C(0.46)a parts per thousand yenT(0.11)a parts per thousand yenB(0.076). Morphine (M), oxycodone (O), t...hebacon (T) and 6,14-ethenomorphinan-7-methanol, 4,5-epoxy-6-fluoro-3-hydroxy-alpha,alpha,17-trimethyl-, (5 alpha,7 alpha) (E) also produced dose-dependent increase in antinociception and hyperthermia. Among morphine derivatives the relative order of analgesic potency was: E(56) gt O(5)a parts per thousand yenT(2.6) gt M(1), and similar to this, the relative order of hyperthermic potency was: E(37) gt O(3)a parts per thousand yenT(2.3) gt M(1). Morphine (phenanthrene-type) and fentanyl (4-anilinopiperidine-type) derivatives produced hyperthermia in rats at doses about 2 times lower, and 6-11 times higher, than their median antinociceptive doses, respectively. This study is first to identify difference between these two classes of opioid drugs in their potencies in producing hyperthermia. Further studies are needed to clarify the significance of these findings.
Keywords:
Fentanyl / Morphine / Derivatives / Temperature / Antinociception / RatsSource:
Archives of Pharmacal Research, 2013, 36, 4, 501-508Publisher:
- Pharmaceutical Soc Korea, Seoul
Funding / projects:
- Basic and Clinical Pharmacological research of mechanisms of action and drug interactions in nervous and cardiovascular system (RS-MESTD-Basic Research (BR or ON)-175023)
DOI: 10.1007/s12272-013-0072-z
ISSN: 0253-6269
WoS: 000317969800014
Scopus: 2-s2.0-84877875097
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Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Vujovic, Katarina R. Savic AU - Vuckovic, Sonja AU - Srebro, Dragana AU - Ivanović, Milovan AU - Došen-Mićović, Ljiljana AU - Vucetic, Cedomir AU - Dzoljic, Eleonora AU - Prostran, Milica PY - 2013 UR - https://cherry.chem.bg.ac.rs/handle/123456789/1633 AB - In addition to producing antinociception, opioids exert profound effects on body temperature. This study aimed at comparing antinociceptive and hyperthermic responses between two groups of mu-opioid receptor agonists: fentanyl (4-anilinopiperidine-type) and morphine (phenanthrene-type) derivatives in rats. Analgesic activity was assessed by tail immersion test and the body temperature by insertion of a thermometer probe into the colon. Fentanyl (F), (+/-)-cis-3-methyl fentanyl (CM), (+/-)-cis-3-carbomethoxy fentanyl (C), (+/-)trans-3-carbomethoxy fentanyl (T) and (+/-)-cis-3 butyl fentanyl (B) produced dose-dependent increase in antinociception and hyperthermia. The relative order of analgesic potency was: CM(11.27) gt F(1) gt C(0.35)a parts per thousand yenT(0.11)a parts per thousand yenB(0.056). Similar to this, the relative order of hyperthermic potency was: CM(8.43) gt F(1) gt C(0.46)a parts per thousand yenT(0.11)a parts per thousand yenB(0.076). Morphine (M), oxycodone (O), thebacon (T) and 6,14-ethenomorphinan-7-methanol, 4,5-epoxy-6-fluoro-3-hydroxy-alpha,alpha,17-trimethyl-, (5 alpha,7 alpha) (E) also produced dose-dependent increase in antinociception and hyperthermia. Among morphine derivatives the relative order of analgesic potency was: E(56) gt O(5)a parts per thousand yenT(2.6) gt M(1), and similar to this, the relative order of hyperthermic potency was: E(37) gt O(3)a parts per thousand yenT(2.3) gt M(1). Morphine (phenanthrene-type) and fentanyl (4-anilinopiperidine-type) derivatives produced hyperthermia in rats at doses about 2 times lower, and 6-11 times higher, than their median antinociceptive doses, respectively. This study is first to identify difference between these two classes of opioid drugs in their potencies in producing hyperthermia. Further studies are needed to clarify the significance of these findings. PB - Pharmaceutical Soc Korea, Seoul T2 - Archives of Pharmacal Research T1 - A comparison of the antinociceptive and temperature responses to morphine and fentanyl derivatives in rats VL - 36 IS - 4 SP - 501 EP - 508 DO - 10.1007/s12272-013-0072-z ER -
@article{ author = "Vujovic, Katarina R. Savic and Vuckovic, Sonja and Srebro, Dragana and Ivanović, Milovan and Došen-Mićović, Ljiljana and Vucetic, Cedomir and Dzoljic, Eleonora and Prostran, Milica", year = "2013", abstract = "In addition to producing antinociception, opioids exert profound effects on body temperature. This study aimed at comparing antinociceptive and hyperthermic responses between two groups of mu-opioid receptor agonists: fentanyl (4-anilinopiperidine-type) and morphine (phenanthrene-type) derivatives in rats. Analgesic activity was assessed by tail immersion test and the body temperature by insertion of a thermometer probe into the colon. Fentanyl (F), (+/-)-cis-3-methyl fentanyl (CM), (+/-)-cis-3-carbomethoxy fentanyl (C), (+/-)trans-3-carbomethoxy fentanyl (T) and (+/-)-cis-3 butyl fentanyl (B) produced dose-dependent increase in antinociception and hyperthermia. The relative order of analgesic potency was: CM(11.27) gt F(1) gt C(0.35)a parts per thousand yenT(0.11)a parts per thousand yenB(0.056). Similar to this, the relative order of hyperthermic potency was: CM(8.43) gt F(1) gt C(0.46)a parts per thousand yenT(0.11)a parts per thousand yenB(0.076). Morphine (M), oxycodone (O), thebacon (T) and 6,14-ethenomorphinan-7-methanol, 4,5-epoxy-6-fluoro-3-hydroxy-alpha,alpha,17-trimethyl-, (5 alpha,7 alpha) (E) also produced dose-dependent increase in antinociception and hyperthermia. Among morphine derivatives the relative order of analgesic potency was: E(56) gt O(5)a parts per thousand yenT(2.6) gt M(1), and similar to this, the relative order of hyperthermic potency was: E(37) gt O(3)a parts per thousand yenT(2.3) gt M(1). Morphine (phenanthrene-type) and fentanyl (4-anilinopiperidine-type) derivatives produced hyperthermia in rats at doses about 2 times lower, and 6-11 times higher, than their median antinociceptive doses, respectively. This study is first to identify difference between these two classes of opioid drugs in their potencies in producing hyperthermia. Further studies are needed to clarify the significance of these findings.", publisher = "Pharmaceutical Soc Korea, Seoul", journal = "Archives of Pharmacal Research", title = "A comparison of the antinociceptive and temperature responses to morphine and fentanyl derivatives in rats", volume = "36", number = "4", pages = "501-508", doi = "10.1007/s12272-013-0072-z" }
Vujovic, K. R. S., Vuckovic, S., Srebro, D., Ivanović, M., Došen-Mićović, L., Vucetic, C., Dzoljic, E.,& Prostran, M.. (2013). A comparison of the antinociceptive and temperature responses to morphine and fentanyl derivatives in rats. in Archives of Pharmacal Research Pharmaceutical Soc Korea, Seoul., 36(4), 501-508. https://doi.org/10.1007/s12272-013-0072-z
Vujovic KRS, Vuckovic S, Srebro D, Ivanović M, Došen-Mićović L, Vucetic C, Dzoljic E, Prostran M. A comparison of the antinociceptive and temperature responses to morphine and fentanyl derivatives in rats. in Archives of Pharmacal Research. 2013;36(4):501-508. doi:10.1007/s12272-013-0072-z .
Vujovic, Katarina R. Savic, Vuckovic, Sonja, Srebro, Dragana, Ivanović, Milovan, Došen-Mićović, Ljiljana, Vucetic, Cedomir, Dzoljic, Eleonora, Prostran, Milica, "A comparison of the antinociceptive and temperature responses to morphine and fentanyl derivatives in rats" in Archives of Pharmacal Research, 36, no. 4 (2013):501-508, https://doi.org/10.1007/s12272-013-0072-z . .