Page last updated: 2024-11-13

2'-hydroxy-5,9-dimethyl-2-allyl-6,7-benzomorphan

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

Description

SK&F 10047: pharmacologic action of cpd may depend on (L)- or (D)-isomerism; RN given refers to cpd without isomeric designation [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID56840988
MeSH IDM0058971

Synonyms (8)

Synonym
2,6-methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(2-propenyl)-, (2r-(2alpha,6alpha,11r*))-
unii-k9dgj27jkh
l-n-allylnormetazocine
2,6-methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(2-propenyl)-, (2r,6r,11r)-
(-)-skf 10.047
(-)-anmc
n-allylnorcyclazocine
sk&f 10047

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"3 microM and 9 microM, respectively, against the toxic action of 100 microM glutamate."( Excitatory amino acid neurotoxicity at the N-methyl-D-aspartate receptor in cultured neurons: protection by SKF 10,047.
Feuerstein, G; Lysko, PG, 1990
)
0.28

Compound-Compound Interactions

ExcerptReferenceRelevance
" The STR was mimicked in mice treated with BD 1047 (a putative σ(1) receptor antagonist), but not SM-21, a putative σ(2) receptor antagonist, in combination with METH."( Straub tail reaction in mice treated with σ(1) receptor antagonist in combination with methamphetamine.
Hall, FS; Kitanaka, J; Kitanaka, N; Nishiyama, N; Takemura, M; Tanaka, K; Uhl, GR, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
"L-745,870,(3-([4-(4-chlorophenyl)piperazin-1-yl]methyl)-1H- pyrollo[2,3-b] pyridine, was identified as a selective dopamine D4 receptor antagonist with excellent oral bioavailability and brain penetration."( Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor.
Baskin, E; Bristow, LJ; Chapman, KL; Curtis, N; Emms, F; Fletcher, AE; Freedman, S; Graham, M; Knowles, M; Kulagowski, JJ; Leeson, PD; Lynch, JJ; Marwood, R; Matheson, S; Mcallister, G; Myers, J; Patel, S; Ragan, CI; Rathbone, D; Ridgill, M; Rupniak, NM; Watt, AP, 1997
)
0.3

Dosage Studied

ExcerptRelevanceReference
" 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
" These results were confirmed by studies employing a self- and cross-displacement design and dose-response surfaces for SKF and TCP, with and without blockade by haloperidol of the sigma site."( Quantitative characterization of multiple binding sites for phencyclidine and N-allylnormetazocine in membranes from rat and guinea pig brain.
Katki, AG; Munson, PJ; Rodbard, D; Schwarz, S; Zhou, GZ, 1991
)
0.28
" In Long-Evans rats, BW942C produced a biphasic dose-response curve for urine output with lower doses increasing and higher doses suppressing output."( Kappa opioid partial agonist activity of the enkephalin-like pentapeptide BW942C based on urination and in vitro studies in humans and animals.
Cone, EJ; Johnson, RE; Su, TP; Vaupel, DB, 1990
)
0.28
" This property was reflected by a greater extent of inhibition of the binding of PCP-selective relative to sigma H-selective ligands at a given cation concentration, as well as by lower IC50's and by steeper slopes of the cation dose-response curves."( Differential modulation by cations of sigma and phencyclidine binding sites in rat brain.
Katki, AG; Rodbard, D; Schwarz, S; Zhou, GZ, 1990
)
0.28
" Dose-response curves for the relatively specific ligands for the mu-, kappa-, and sigma-receptors were determined using morphine (mu-receptors), dynorphin-(1-13) (kappa-receptors), and N-allylnormetazocine (sigma-receptors)."( Sites of action of mu-, kappa- and sigma-opiate receptor agonists at the feline ileocecal sphincter.
Cohen, S; Ouyang, A; Vos, P, 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
" Comparisons of dose-response curves and efficacies demonstrated that d-NANM was more similar to PCP in its effectiveness in depressing the flexor and skin twitch reflexes than was l-NANM."( Pharmacologic and reinforcing properties of phencyclidine and the enantiomers of N-allylnormetazocine in the dog.
Risner, ME; Shannon, HE; Vaupel, DB, 1986
)
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
"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
" Dose-response determinations were made for responses to phencyclidine, to a racemic mixture of N-allylnormetazocine, and to the pure levo and dextro isomers of N-allylnormetazocine."( Stereoisomers of N-allylnormetazocine: phencyclidine-like behavioral effects in squirrel monkeys and rats.
Balster, RL; Brady, KT; May, EL, 1982
)
0.26
" Comparisons were made on the basis of dose-response relationships."( Anorexia and hyperphagia produced by five pharmacologic classes of hallucinogens.
Morton, EC; Vaupel, DB, 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
" In the present work, using whole-cell patch-clamp techniques in rat retinal slice preparations, we further demonstrate that SKF of higher dosage (50μM) significantly suppressed AMPA receptor (AMPAR)-mediated light-evoked excitatory postsynaptic currents (L-EPSCs) of retinal ON-type GCs (ON GCs), and the effect was reversed by the σR1 antagonist BD1047, suggesting the involvement of σR1."( Activation of the sigma receptor 1 modulates AMPA receptor-mediated light-evoked excitatory postsynaptic currents in rat retinal ganglion cells.
Deng, QQ; Liu, LL; Weng, SJ; Yang, XL; Zhong, YM, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (395)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990192 (48.61)18.7374
1990's143 (36.20)18.2507
2000's39 (9.87)29.6817
2010's19 (4.81)24.3611
2020's2 (0.51)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.21

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index8.21 (24.57)
Research Supply Index6.02 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews11 (2.69%)6.00%
Case Studies1 (0.24%)4.05%
Observational0 (0.00%)0.25%
Other397 (97.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]