Page last updated: 2024-12-06

cyclazocine

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Description

Cyclazocine is a synthetic opioid analgesic, chemically related to morphine. It was synthesized in the 1960s and initially investigated as a potential treatment for pain, but its use has been limited due to its complex pharmacological profile. Cyclazocine acts as a mixed opioid agonist-antagonist, meaning it can both activate and block opioid receptors in the brain. As an agonist, it produces analgesic effects and can induce euphoria, but as an antagonist, it can block the effects of other opioids, such as heroin. This mixed action makes cyclazocine useful in treating opioid addiction, as it can reduce withdrawal symptoms while blocking the euphoric effects of heroin. However, cyclazocine can also cause a variety of side effects, including nausea, vomiting, dizziness, and hallucinations. Its potential for abuse and the availability of safer alternatives have led to its limited use in clinical practice. Researchers continue to study cyclazocine for its potential applications in pain management, addiction treatment, and neuroprotection. The complex interplay of its agonist and antagonist properties makes cyclazocine a valuable tool for understanding opioid receptor function and the development of novel therapeutic strategies.'

Cyclazocine: An analgesic with mixed narcotic agonist-antagonist properties. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID19143
CHEMBL ID289683
SCHEMBL ID37996
MeSH IDM0005452

Synonyms (70)

Synonym
nsc172134
2, 3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-, (2.alpha.,6.alpha.,11r*)-
nsc-172134
2,6-methano-3-benzazocin-8-ol, 3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-
3-(cyclopropylmethyl)-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-8-ol
3-cyclopropylmethyl-6(eq),11(ax)-dimethyl-2,6-methano-3-benzazocin-8-ol
2,6-methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-3-(cyclopropylmethyl)-6,11-dimethyl-
cyclazocine [usan:inn]
einecs 222-689-9
2-cyclopropylmethyl-5,9-dimethyl-2'-hydroxy-6,7-benzomorphan
nsc 107429
ciclazocina [inn-spanish]
3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-2,6-methano-3-benzazocin-8-ol
cyclazocinum [inn-latin]
2-cyclopropylmethyl-5,9-dimethyl-2'-hydroxy-6,7-beneomorphan
3-(cyclopropylmethyl)1-1,2,3,4,5,6-hexahydro-6,11-dimethyl-2, 6-methano-3-benzazocin-8-ol
3-(cyclopropylmethyl)-1,2,3, 4,5,6-hexahydro-6,11-dimethyl-2,6-methano-3-benzazocin-8-ol
2, 6-methano-3-benzazocin-8-ol, 1,2,3,4,5, 6-hexahydro-3-(cyclopropylmethyl)-6,11-dimethyl-
2-cyclopropylmethyl-2'-hydroxy-5,9-dimethyl-6,7-benzomorphan
2, 6-methano-3-benzazocin-8-ol, 3-(cyclopropylmethyl)-1,2,3,4,5, 6-hexahydro-6,11-dimethyl-
cyclopropylmethyl(dimethyl)[?]ol
{3-cyclopropylmethyl-6[eq],} {11[ax]-dimethyl-2,6-methano-3-benzazocin-8-ol}
D03618
cyclazocine (usan/inn)
3-(cyclopropylmethyl)-1,3,4,5,6-hexahydro-6,11-dimethyl-2,6-methano-3-benzazocin-8-ol
um 407
3-(cyclopropylmethyl)1-1,3,4,5,6-hexahydro-6,11-dimethyl-2,6-methano-3-benzazocin-8-ol
3572-80-3
2-cyclopropylmethyl-5,7-beneomorphan
wln: t c666 a kn&ttj a1 b1 eq k1- al3tj
nsc107429
nih 7981
cyclazocine
2-cyclopropylmethyl-2'-hydroxy-5,7-benzomorphan
win 20,740
2, 3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-
win 20740
3-cyclopropylmethyl-6[eq],6-methano-3-benzazocin-8-ol
mls002703971 ,
2, 1,2,3,4,5,6-hexahydro-3-(cyclopropylmethyl)-6,11-dimethyl-
nsc-107429
L001209
FT-0665329
cyclazocine (-)
cyclazocine (+)
(cyclazocine) 3-cyclopropylmethyl-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocin-8-ol
bdbm50018731
rac-cyclazocine
CHEMBL289683
(+/-)-cyclazocine
smr001395644
unii-j5w1b1159c
j5w1b1159c ,
ciclazocina
cyclazocinum
(2alpha,6alpha,11r*)-(1)-3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-2,6-methano-3-benzazocin-8-ol
7346-09-0
einecs 230-866-7
cyclazocine [mi]
cyclazocine [inn]
cyclazocine [usan]
SCHEMBL37996
YQYVFVRQLZMJKJ-UHFFFAOYSA-N
DTXSID9022863
2,6-methano-3-benzazocin-8-ol, 3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-; cyclazocine; nsc 107429; win 20740
Q5198126
10-(cyclopropylmethyl)-1,13-dimethyl-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol
3,4,5,6-tetrachloro-phthalic acid
FT-0665328
2,6-methano-3-benzazocin-8-ol,3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-,(2s,6s,11s)-

Research Excerpts

Overview

Cyclazocine is a mu opioid antagonist and kappa opioid agonist. It was studied in the 1960s as a potential treatment for heroin addicts.

ExcerptReferenceRelevance
"Cyclazocine is a kappa-opioid receptor agonist and mu-opioid receptor antagonist that was studied in the 1960s as a potential treatment for heroin addicts. "( Effects of cyclazocine on cocaine self-administration in rats.
Glick, SD; Maisonneuve, IM; Visker, KE, 1998
)
2.13
"(+/-)Cyclazocine is a mu opioid antagonist and kappa opioid agonist, and because of these actions, would be expected to modulate dopamine release in the nucleus accumbens as well as the reinforcing effects of drugs of abuse."( (+/-)Cyclazocine blocks the dopamine response to nicotine.
Glick, SD; Maisonneuve, IM, 1999
)
1.27
"Cyclazocine is a low-liability analgesic and potential therapeutic for the treatment of drug abuse."( Partial opioids. Medications for the treatment of pain and drug abuse.
Bidlack, JM; McLaughlin, JP; Wentland, MP, 2000
)
1.03
"Ketocyclazocine thus appears to be a selective agonist at the kappa receptor."( The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
Eades, CG; Gilbert, PE; Huppler, RE; Martin, WR; Thompson, JA, 1976
)
0.74
"Cyclazocine is a mu antagonist and mixed kappa and sigma agonist."( The effects of morphine and nalorphine-like drugs in the nondependent, morphine-dependent and cyclazocine-dependent chronic spinal dog.
Gilbert, PE; Martin, WR, 1976
)
1.2
"Cyclazocine is a benzomorphan derivative, considered as a mixed kappa and and sigma opioid receptor agonist. "( [The role of serotonin in the behavioral changes induced in the rat by cyclazocine].
Gavend, M; Gavend, MR; Serre-Debeauvais, F,
)
1.81
"Cyclazocine is a benzomorphan which, in addition to more classical opiate properties, binds to the sigma opiate receptor site. "( Electrophysiological effects of cyclazocine on rat cerebellar Purkinje neurons: comparison with phencyclidine.
Freedman, R; Kim, M; Palmer, M; Pang, K,
)
1.86

Bioavailability

ExcerptReferenceRelevance
" In an attempt to synthesize analogs of cyclazocine with increased bioavailability and varying kappa agonist and partial mu agonist properties, a series of 8-amino derivatives of cyclazocine were synthesized."( Partial opioids. Medications for the treatment of pain and drug abuse.
Bidlack, JM; McLaughlin, JP; Wentland, MP, 2000
)
0.57

Dosage Studied

Tolerance to the behavioral effects of selected opiate compounds was evaluated using cumulative dosing procedures in rhesus monkeys responding under a fixed-ratio schedule of food presentation. After reliable discriminative control of lever choice was established, dose-response determinations were made.

ExcerptRelevanceReference
" Unfortunately, the occurrence of psychotomimetic side effects prevented the administration of doses of Win 20,836 equieffective with the morphine standard, and this necessitated substantal extrapolation of the dose-response curve of the test drug to arrive at a relative potency estimate."( Twin crossover relative potency analgesic assays in man. II. Morphine vs. 8-methoxycyclazocine.
Beaver, WT; Feise, GA,
)
0.36
" Naloxone (5-500 microgram/kg) uniformly produced a dose dependent, parallel shift of the morphine dose-response curves to right."( A dose ratio comparison of the interaction between morphine and cyclazocine with naloxone in rhesus monkeys on the shock titration task.
Rudy, TA; Yaksh, TL, 1977
)
0.5
" These studies were carried out with a twice-a-day dosage regimen."( Naltrexone and cyclazocine. A controlled treatment study.
Brahen, LS; Capone, T; Desiderio, D; Wiechert, V, 1977
)
0.61
" Dose-response curves were determined for the effects of morphine (0."( Comparison of the effects of morphine, pentazocine, cyclazocine and amphetamine on intracranial self-stimulation in the rat.
Holtzman, SG, 1976
)
0.51
" When ischemic animals were administered the multiple dosing regimen of (+)SKF 10,047, no hypothermic effect was noted in the temporalis muscle over 4 hours' postischemia."( Neuroprotective effects of SKF 10,047 in cultured rat cerebellar neurons and in gerbil global brain ischemia.
Feuerstein, G; Gagnon, RC; Gu, JL; Lysko, PG; Yue, TL, 1992
)
0.28
" 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
)
0.5
"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
)
0.47
"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
)
0.73
" Rats were dosed continuously with morphine hydrochloride by giving a daily dose through tubes connected to small, subcutaneously implanted reservoirs."( An implanted reservoir of morphine solution for rapid induction of physical dependence in rats.
Goode, PG, 1971
)
0.25
") 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
)
0.51
" 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
" After reliable discriminative control of lever choice was established, dose-response determinations for generalization to the training dose of PCP were made with several doses of PCP, a racemic mixture of cyclazocine and the pure (+)- and (-)-isomers of cyclazocine."( Discriminative stimulus properties of stereoisomers of cyclazocine in phencyclidine-trained squirrel monkeys.
Balster, RL; Brady, KT, 1982
)
0.7
" 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
)
0.56
" 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
)
1.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorHomo sapiens (human)Ki0.00020.00000.419710.0000AID719453
Delta-type opioid receptorHomo sapiens (human)Ki0.00200.00000.59789.9300AID719452
Kappa-type opioid receptorHomo sapiens (human)Ki0.00010.00000.362410.0000AID719305
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID1382963Displacement of [3H]DAMGO from MOR in guinea pig brain membranes after 60 mins by scintillation counting method2018European journal of medicinal chemistry, Mar-25, Volume: 148Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.
AID719303Selectivity ratio of Ki for human kappa opioid receptor to Ki for human mu opioid receptor2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.
AID719453Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.
AID1382964Displacement of [3H]Naltrindole from DOR in guinea pig brain membranes after 3 hrs by scintillation counting method2018European journal of medicinal chemistry, Mar-25, Volume: 148Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.
AID1382965Displacement of [3H]U69,593 from KOR in guinea pig brain membranes after 60 mins by scintillation counting method2018European journal of medicinal chemistry, Mar-25, Volume: 148Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.
AID719452Displacement of [3H]Naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.
AID719305Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.
AID719304Selectivity ratio of Ki for human delta opioid receptor to Ki for human mu opioid receptor2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.
AID493017Wombat Data for BeliefDocking2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
8-Aminocyclazocine analogues: synthesis and structure-activity relationships.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (810)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990727 (89.75)18.7374
1990's53 (6.54)18.2507
2000's23 (2.84)29.6817
2010's6 (0.74)24.3611
2020's1 (0.12)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 45.31

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index45.31 (24.57)
Research Supply Index6.79 (2.92)
Research Growth Index4.02 (4.65)
Search Engine Demand Index76.15 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (45.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials30 (3.51%)5.53%
Reviews29 (3.39%)6.00%
Case Studies1 (0.12%)4.05%
Observational0 (0.00%)0.25%
Other795 (92.98%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]