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ethylketocyclazocine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

Ethylketocyclazocine: A kappa opioid receptor agonist. The compound has analgesic action and shows positive inotropic effects on the electrically stimulated left atrium. It also affects various types of behavior in mammals such as locomotion, rearing, and grooming. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135018
MeSH IDM0024932

Synonyms (14)

Synonym
gtpl1610
ethyketazocine
(+/-)-ekc
(plusmn)-ethylketazocine
(1r,9r,13s) ethyketazocine
win-35,197-2
PDSP2_001345
PDSP2_001344
6036-52-8
ekc
ethylketocyclazocine
DTXSID70276356
Q27077240
(1r,9r,13s)-10-(cyclopropylmethyl)-1-ethyl-4-hydroxy-13-methyl-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-8-one

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" When given in combination with cocaine, EKC produced effects that were sub-additive, suggesting that the kappa agonists may be used safely as cocaine abuse treatments."( Effects of kappa opioid agonists alone and in combination with cocaine on heart rate and blood pressure in conscious squirrel monkeys.
Bergman, J; Gilman, JP; Goldberg, SR; Graczyk, Z; Mello, NK; Negus, SS; Schindler, CW, 2007
)
0.34

Dosage Studied

Kappa agonists, including bremazocine, tifluadom, ethylketocyclazocines, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves.

ExcerptRelevanceReference
" Within regions intermediate between the dorsal posterior, mesencephalic tegmentum and posterior medulla, (-)-nicotine produced biphasic dose-response and time action curves."( Opioid and nicotinic analgesic and hyperalgesic loci in the rat brain stem.
Hamann, SR; Martin, WR, 1992
)
0.28
" The mean digoxin dosage at the development of fatal arrhythmias after the 100 micrograms/kg of FK 33,824 was 30% lower than the control group."( Opioid receptor agonists D-Ala-2-Me-Phe-4-Met-(O)-ol enkephalin and ethylketocyclazocine in the brain accentuate digoxin-induced arrhythmias.
Rabkin, SW,
)
0.13
" Flumazenil (Ro 15-1788) administration caused a parallel shift to the right of the dose-response curve for midazolam spinal analgesia."( On the mechanism by which midazolam causes spinally mediated analgesia.
Edwards, M; Gent, JP; Goodchild, CS; Serrao, JM, 1990
)
0.28
" The return to normal naltrexone sensitivity after elimination of the two highest doses suggests that a reliable association between the lower and higher doses in a cumulative dosing procedure can result in conditioned effects to the lower doses."( Enhanced sensitivity to behavioral effects of naltrexone in rats.
Goldberg, SR; Katz, JL; Schindler, CW; Su, TP; Wu, XZ, 1990
)
0.28
" However, the dose-response curve for naltrexone was not parallel to the morphine or fentanyl dose-response curves."( An analysis of naltrexone and naloxone's possible agonistic actions in the dog.
Martin, WR; Wettstein, JG, 1985
)
0.27
" Similar blockade was observed for EKC and U 50488 at doses of 10 and/or 20 ng/kg, but DAGO was unable to affect the AS-induced gastric inhibition at any dosage tested (20-200 ng/kg icv)."( CNS blockade of acoustic stress-induced gastric motor inhibition by kappa-opiate agonists in dogs.
Alvinerie, M; Bueno, L; Gue, M; Honde, C; Junien, JL; Pascaud, X, 1988
)
0.27
" Complete dose-response data for morphine, heroin, etorphine, d- and l-ethylketazocine, d- and l-pentazocine, and d- and l-N-allylnormetazocine revealed a predominant response of hyperthermia."( Body temperature effects of opioids in rats: intracerebroventricular administration.
Adler, MW; Geller, EB; Rowan, CH, 1986
)
0.27
" The administration of the lowest dose of EKC stimulated the release of prolactin whereas higher doses were without effect suggesting biphasic dose-response relationship."( Identification of multiple opiate receptors through neuroendocrine responses. I. Effects of agonists.
George, R; Pechnick, R; Poland, RE, 1985
)
0.27
" But a number of kappa agonists, including bremazocine, tifluadom, ethylketocyclazocine, ketocyclazocine, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves."( Profile of activity of kappa receptor agonists in the rabbit vas deferens.
Hayes, A; Kelly, A, 1985
)
0.27
"Systemic administration of beta-funaltrexamine (beta-FNA) 24 hr before analgesic testing produced approximately a 10-fold parallel shift in the dose-response curves of the prototypic mu agonists morphine, I-methadone, fentanyl and etorphine in the mouse abdominal constriction test."( Use of beta-funaltrexamine to determine mu opioid receptor involvement in the analgesic activity of various opioid ligands.
Hynes, MD; Leander, JD; Reel, JK; Zimmerman, DM, 1987
)
0.27
" After 12 generations of selective breeding, the high antinociceptive response line exhibited about 7 times steeper dose-response curve than did the low antinociceptive response line whereas only small differences were seen with saline alone."( Selective breeding for levorphanol-induced antinociception on the hot-plate assay: commonalities in mechanism of action with morphine, pentazocine, ethylketocyclazocine, U-50488H and clonidine in mice.
Belknap, JK; Danielson, PW; Laursen, SE; Noordewier, B, 1987
)
0.27
"Tolerance to the behavioral effects of selected opiate compounds (cyclazocine, ketocyclazocine, naloxone and the stereoisomers of N-allylnormetazocine) and phencyclidine was evaluated using cumulative dosing procedures in rhesus monkeys responding under a fixed-ratio (FR) schedule of food presentation."( Behavioral effects of selected opiates and phencyclidine in the nondependent and cyclazocine-dependent rhesus monkey.
Bergman, J; Hassoun, J; Schuster, CR, 1985
)
0.27
") produced a dose-response curve with a reduced maximum effect."( Relative involvement of receptor subtypes in opioid-induced inhibition of intestinal motility in mice.
Takemori, AE; Ward, SJ,
)
0.13
" Although the group X dosage interaction was not significant, an internally consistent tendency effect of naloxone among the different treatment groups was observed."( The effect of ovariectomy, estradiol and progesterone on opioid modulation of feeding.
Gosnell, BA; Grace, M; Kneip, J; Levine, AS; Morley, JE, 1984
)
0.27
"3 mg/kg) produced a 3-fold shift to the right of the cyclazocine dose-response curve but did not completely block the cyclazocine-like stimulus effects of either SKF 10,047 or ethylketocyclazocine."( Discriminative stimulus effects of prototype opiate receptor agonists in monkeys.
Holtzman, SG; Teal, JJ, 1980
)
0.26
" Parallel dose-response lines were obtained for the two opioid agonists but the effect of EKC was more resistant to naloxone antagonism."( Mu and kappa opioid agonists elevate brain stimulation threshold for escape by inhibiting aversion.
Bonnet, KA; Carr, KD; Simon, EJ, 1982
)
0.26
" Dose-response curves were plotted with naloxone against the changes produced by each agonist, and the effect of a number of anticonvulsant drugs on agonist-induced seizures was ascertained."( The epileptogenic spectrum of opiate agonists.
Bearden, LJ; Snead, OC, 1982
)
0.26
"0 mg/kg) produced dose-related shifts to the right in the dose-response curves for the discriminative stimulus and rate-decreasing effects of morphine and ethylketazocine without affecting the response produced by meperidine."( Narcotic discrimination in pigeons: antagonism by naltrexone.
Herling, S; Solomon, RE; Valentino, RJ; Woods, JH, 1984
)
0.27
" Footshock intensity thresholds for eliciting locomotion were determined and dose-response curves for EKC and MS analgesia were obtained."( Analgesic effects of ethylketocyclazocine and morphine in rat and toad.
Aleman, DO; Carr, KD; Holland, MJ; Simon, EJ, 1984
)
0.27
" Ketocyclazocine dose-response functions were determined for each monkey under their original training conditions and then the conditions were reversed and dose-response functions were re-determined under the new conditions."( Effects of ketocyclazocine alone and in combination with naloxone on schedule-controlled responding in squirrel monkeys.
Dykstra, LA; Milar, KS, 1983
)
0.27
" Naloxone (1 microM) or norbinaltorphimine (10 nM) shifted the dose-response curve of (-)-U50,488H to the right by 100-fold."( Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Chen, C; Li, JG; Liu-Chen, LY; Luo, LY; Zhu, J, 1997
)
0.3
" In dose-response tests, subjects rarely responded on the U-50,488H-appropriate key when morphine was administered or on the morphine-appropriate key when they received U-50,488H."( Establishing morphine and U-50,488H as discriminative stimuli in a three-choice assay with pigeons.
Makhay, MM; Poling, A; Young, AM, 1998
)
0.3
" Dose-response curves were generally quantal under the FR and graded under the FI schedules, but highly variable among subjects under the FI."( Drug discrimination in pigeons trained to discriminate among morphine, U50488, a combination of these drugs, and saline.
Li, M; McMillan, DE; Wessinger, WD, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1346329Human kappa receptor (Opioid receptors)1997The Journal of pharmacology and experimental therapeutics, Aug, Volume: 282, Issue:2
Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
AID1346373Mouse delta receptor (Opioid receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Jul-15, Volume: 90, Issue:14
Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
AID1346341Mouse kappa receptor (Opioid receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Jul-15, Volume: 90, Issue:14
Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
AID1346411Rat kappa receptor (Opioid receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21
Cloning and pharmacological characterization of a rat kappa opioid receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (529)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990407 (76.94)18.7374
1990's107 (20.23)18.2507
2000's12 (2.27)29.6817
2010's3 (0.57)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (0.54%)5.53%
Reviews7 (1.25%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other549 (98.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]