Levorphanol
Morphinans
Receptors, sigma
A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.
Phenazocine
Pentazocine
Biometric Identification
A method of differentiating individuals based on the analysis of qualitative or quantitative biological traits or patterns. This process which has applications in forensics and identity theft prevention includes DNA profiles or DNA fingerprints, hand fingerprints, automated facial recognition, iris scan, hand geometry, retinal scan, vascular patterns, automated voice pattern recognition, and ultrasound of fingers.
Tripelennamine
Carisoprodol
A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202)
Orphenadrine
Hydroxyzine
Nefopam
Amitriptyline
Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.
Hydromorphone
Hydrocodone
Oxymorphone
An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)
Analgesics, Opioid
Miosis
Codeine
PubMed
A bibliographic database that includes MEDLINE as its primary subset. It is produced by the National Center for Biotechnology Information (NCBI), part of the NATIONAL LIBRARY OF MEDICINE. PubMed, which is searchable through NLM's Web site, also includes access to additional citations to selected life sciences journals not in MEDLINE, and links to other resources such as the full-text of articles at participating publishers' Web sites, NCBI's molecular biology databases, and PubMed Central.
Publishing
MEDLINE
Serial Publications
Biological Science Disciplines
All of the divisions of the natural sciences dealing with the various aspects of the phenomena of life and vital processes. The concept includes anatomy and physiology, biochemistry and biophysics, and the biology of animals, plants, and microorganisms. It should be differentiated from BIOLOGY, one of its subdivisions, concerned specifically with the origin and life processes of living organisms.
Organophosphonates
Amination
Molecular Structure
Phosphorus
Structure-Activity Relationship
Stereoisomerism
Fentanyl
Morphine
Drug Tolerance
Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.
Acetaminophen
Analgesics, Non-Narcotic
Meptazinol
Levallorphan
An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)
Activation of peripheral kappa opioid receptors inhibits capsaicin-induced thermal nociception in rhesus monkeys. (1/80)
8-Methyl-N-vanillyl-6-nonenamide (capsaicin) was locally applied in the tail of rhesus monkeys to evoke a nociceptive response, thermal allodynia, which was manifested as reduced tail-withdrawal latencies in normally innocuous 46 degrees C water. Coadministration of three kappa opioid ligands, U50,488 (3.2-100 microgram), bremazocine (0.1-3.2 microgram), and dynorphin A(1-13) (3.2-100 microgram), with capsaicin in the tail dose-dependently inhibited capsaicin-induced allodynia. This local antinociception was antagonized by a small dose of an opioid antagonist, quadazocine; (0.32 mg), applied in the tail; however, this dose of quadazocine injected s.c. in the back did not antagonize local U50,488. Comparing the relative potency of either agonist or antagonist after local and systemic administration confirmed that the site of action of locally applied kappa opioid agonists is in the tail. In addition, local nor-binaltorphimine (0.32 mg) and oxilorphan (0.1-10 microgram) antagonist studies raised the possibility of kappa opioid receptor subtypes in the periphery, which indicated that U50,488 produced local antinociception by acting on kappa1 receptors, but bremazocine acted probably on non-kappa1 receptors. These results provide functional evidence that activation of peripheral kappa opioid receptors can diminish capsaicin-induced allodynia in primates. This experimental pain model is a useful tool for evaluating peripherally antinociceptive actions of kappa agonists without central side effects and suggests new approaches for opioid pain management. (+info)Characterization of the decrease of extracellular striatal dopamine induced by intrastriatal morphine administration. (2/80)
The effect of intrastriatally-administered morphine on striatal dopamine (DA) release was studied in freely moving rats. Morphine (1, 10 or 100 microM) was given into the striatum by reversed microdialysis, and concentrations of DA and its metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) were simultaneously measured from the striatal dialysates. Intrastriatally-administered morphine significantly and dose-dependently decreased the extracellular concentration of DA, the concentrations of the acidic DA metabolites were only slightly decreased. The effect of morphine was antagonized by naltrexone (2.25 mg kg(-1), s.c.). Pretreatment with a preferential kappa-opioid receptor antagonist, MR2266 [(-)-5,9 alpha-diethyl-2-(3-furylmethyl)-2'-hydroxy-6,7-benzomorphane; 1 mg kg(-1), s.c.], had no effect on the decrease of extracellular DA evoked by intrastriatal morphine (100 microM). Intrastriatal administration of the selective micro-opioid receptor agonist [D-Ala2,MePhe4,Gly-ol5] enkephalin (DAMGO; 1 microM), significantly decreased the extracellular concentration of DA in the striatum. When the rats were given morphine repeatedly in increasing doses (10-25 mg kg(-1), s.c.) twice daily for 7 days and withdrawn for 48 h, the decrease of extracellular DA induced by morphine (100 microM) was significantly less than that seen in saline-treated controls. Our results show that besides the well-known stimulatory effect there is a local inhibitory component in the action of morphine on striatal DA release in the terminal regions of nigrostriatal DA neurones. Tolerance develops to this inhibitory effect during repeated morphine treatment. Furthermore, our results suggest that the effect of intrastriatally-administered morphine is mediated by the micro-opioid receptors. (+info)Intracisternal nor-binaltorphimine distinguishes central and peripheral kappa-opioid antinociception in rhesus monkeys. (3/80)
Systemic administration of nor-binaltorphimine (nor-BNI) produces a long-lasting kappa-opioid receptor (kappaOR) antagonism and has kappa(1)-selectivity in nonhuman primates. The aim of this study was to establish the pharmacological basis of central kappaOR antagonism in rhesus monkeys (Macaca mulatta). After intracisternal (i.c.) administration of small doses of nor-BNI, the duration and selectivity of nor-BNI antagonism were evaluated against two kappaOR agonists, (trans)-3, 4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide (U50,488) and bremazocine. Thermal antinociception was measured in the warm water (50 degrees C) tail-withdrawal assay and sedation was evaluated by observers blind to treatment conditions. Following i.c. pretreatment with 0.32 mg nor-BNI, a 5- to 10-fold rightward shift of the U50,488 baseline dose-effect curve was observed in antinociception. In contrast, this dose of nor-BNI only produced an insignificant 2-fold shift against bremazocine. Pretreatment with a smaller dose (0.032 mg) of nor-BNI produced a 3-fold shift of U50, 488, which lasted for 7 days, but failed to alter the potency of bremazocine. This differential antagonism profile of i.c. nor-BNI also was observed in sedation ratings. In addition, the centrally effective dose of nor-BNI (0.32 mg), when administered s.c. in the back, did not antagonize either U50,488- or bremazocine-induced antinociception and sedation. After i.c. pretreatment with the same dose, nor-BNI also did not antagonize the peripherally mediated effect of U50,488 against capsaicin-induced thermal nociception in the tail. These results indicate that i.c. nor-BNI produces central kappaOR antagonism and support the notion of two functional kappaOR subtypes in the central nervous system. Moreover, it provides a valuable pharmacological basis for further characterizing different sources of kappaOR-mediated effects, namely, from central or peripheral nervous system receptors. (+info)Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CL. (4/80)
We have synthesized a new benzomorphan derivative, 2R-[2alpha,3(S*), 6alpha]-1,2,3,4,5,6-hexahydro-6,11, 11-trimethyl-3-[2-(phenylmethoxy)propyl]-2, 6-methano-3-benzazocin-10-ol hydrochloride (BIII 890 CL), which displaced [(3)H]batrachotoxinin A-20alpha-benzoate from neurotoxin receptor site 2 of the Na(+) channel in rat brain synaptosomes (IC(50) = 49 nM), but exhibited only low affinity for 65 other receptors and ion channels. BIII 890 CL inhibited Na(+) channels in cells transfected with type IIA Na(+) channel alpha subunits and shifted steady-state inactivation curves to more negative potentials. The IC(50) value for the inactivated Na(+) channel was much lower (77 nM) than for Na(+) channels in the resting state (18 microM). Point mutations F1764A and Y1771A in transmembrane segment S6 in domain IV of the alpha subunit reduced the voltage- and frequency-dependent block, findings which suggest that BIII 890 CL binds to the local anesthetic receptor site in the pore. BIII 890 CL inhibited veratridine-induced glutamate release in brain slices, as well as glutamate release and neurotoxicity in cultured cortical neurons. BIII 890 CL (3-30 mg/kg s.c.) reduced lesion size in mice and rats when administered 5 min after permanent focal cerebral ischemia at doses that did not impair motor coordination. In contrast to many other agents, BIII 890 CL was neuroprotective in both cortical and subcortical regions of the rat brain. Our results demonstrate that BIII 890 CL is a potent, selective, and highly use-dependent Na(+) channel blocker that protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents. (+info)Incomplete, asymmetric, and route-dependent cross-tolerance between oxycodone and morphine in the Dark Agouti rat. (5/80)
Our previous studies indicate that oxycodone is a putative kappa-opioid agonist, whereas morphine is a well documented micro-opioid agonist. Because there is limited information regarding the development of tolerance to oxycodone, this study was designed to 1) document the development of tolerance to the antinociceptive effects of chronically infused i.v. oxycodone relative to that for i. v. morphine and 2) quantify the degree of antinociceptive cross-tolerance between morphine and oxycodone in adult male Dark Agouti (DA) rats. Antinociceptive testing was performed using the tail-flick latency test. Complete antinociceptive tolerance was achieved in 48 to 84 h after chronic infusion of equi-antinociceptive doses of i.v. oxycodone (2.5 mg/24 h and 5 mg/24 h) and i.v. morphine (10 mg/24 h and 20 mg/24 h, respectively). Dose-response curves for bolus doses of i.v. and i.c.v. morphine and oxycodone were produced in naive, morphine-tolerant, and oxycodone-tolerant rats. Consistent with our previous findings that oxycodone and morphine produce their intrinsic antinociceptive effects through distinctly different opioid receptor populations, there was no discernible cross-tolerance when i.c.v. oxycodone was given to morphine-tolerant rats. Similarly, only a low degree of cross-tolerance (approximately 24%) was observed after i.v. oxycodone administration to morphine-tolerant rats. By contrast, both i.v. and i.c.v. morphine showed a high degree of cross-tolerance (approximately 71% and approximately 54%, respectively) in rats rendered tolerant to oxycodone. Taken together, these findings suggest that, after parenteral but not supraspinal administration, oxycodone is metabolized to a mu-opioid agonist metabolite, thereby explaining asymmetric and incomplete cross-tolerance between oxycodone and morphine. (+info)Pharmacological examination of contractile responses of the guinea-pig isolated ileum produced by mu-opioid receptor antagonists in the presence of, and following exposure to, morphine. (6/80)
We have assessed the potential of several mu-opioid receptor antagonists to elicit a response in the guinea-pig isolated ileum in the presence of, and following overnight exposure to, morphine. Naloxone, D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH(2) (CTOP), (-)-5, 9alpha-diethyl-2-(3-furyl-methyl)-2'-hydroxy-6,7-benzomorphan (MR2266), but not D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH(2) (CTAP), produced a transient inhibition of electrically-evoked contractions of the guinea-pig ileum. The effect of 1 microM CTOP, but not that to MR2266, was inhibited by 1 microM somatostatin. Naloxone (0.3 microM), CTOP (3 microM), CTAP (3 microM) and MR2266 (0.3 microM) antagonized the inhibitory effect of morphine on electrically-evoked contractions of the guinea-pig to a similar degree and, following 60 min exposure to morphine, produced non-sustained contractions. The response to 3 microM CTOP was significantly smaller than that to 3 microM CTAP. None of the antagonists produced a response in the absence of morphine. Following overnight exposure of the ileum to 0.3 microM morphine (4 degrees C), and repeated washing to remove the agonist, all four antagonists elicited non-sustained contractions. However, the responses to 3 microM CTOP and 0.3 microM MR2266 were significantly smaller than those elicited by 0.3 microM naloxone and 3 microM CTAP. Somatostatin (1 microM) significantly reduced naloxone-induced contractions, but not those to CTAP. While all four mu-opioid antagonists elicited contractions in the presence of, and following prolonged exposure to, morphine, differences between them were noted which may be a consequence of non-opioid actions. (+info)Dose- and time-dependent bimodal effects of kappa-opioid agonists on locomotor activity in mice. (7/80)
The kappa-opioid agonists U50488H, bremazocine, and BRL52537, and the mu-opioid agonist morphine were compared in their ability to modify spontaneous motor activity in male NMRI mice. Higher, analgesic doses of the kappa-agonists reduced rearing, motility, and locomotion in nonhabituated mice. These effects, as well as the analgesic action of U50488H, were blocked by the selective kappa-opioid antagonists nor-binaltorphimine and DIPPA. In contrast, lower, subanalgesic doses (1.25 and 2.5 mg/kg for U50488H; 0.15 and 0.075 mg/kg for bremazocine, and 0.1 mg/kg for BRL52537) time dependently increased motor activity. The stimulatory effects of U50488H and bremazocine were not observed in habituated animals and were reduced by dopamine depletion. Surprisingly, the stimulatory effects of U50488H and bremazocine were not blocked by nor-binaltorphimine and DIPPA but they were completely eliminated by naloxone (0.1 mg/kg). The effects of morphine were dose-dependent; an initial limited suppression was followed by increased motility and locomotion (but not rearing) with a peak effect at 20 mg/kg both in habituated and nonhabituated mice. The selective mu-opioid antagonist beta-funaltrexamine blocked morphine-induced motor stimulation and analgesia but failed to affect the analgesic and motor stimulatory effects of U50488H. The results indicate that kappa-opioid agonists interact with different functional subtypes of opioid receptors. A stimulatory, naloxone-sensitive but nor-binaltorphimine- and DIPPA-insensitive subtype of opioid receptor appears to operate only when the dopamine system is tonically active in nonhabituated animals. At higher doses, kappa-agonists produce analgesia and motor suppression, effects mediated by a "classic" (inhibitory) kappa-opioid receptor. (+info)kappa-Opioid receptor potentiates apoptosis via a phospholipase C pathway in the CNE2 human epithelial tumor cell line. (8/80)
The mechanism by which kappa-opioid receptor (kappaor) modulated apoptosis was investigated in CNE2 human epithelial tumor cells. Induction of these cells to undergo apoptosis with staurosporine was associated with a massive increase in intracellular cAMP level. The inhibition of the increase in cAMP partially inhibited apoptosis as evidenced by a reduction of PARP and caspase-3 cleavage. Accordingly, a low but significant level of apoptosis is induced in these cells by the elevation of cAMP through the addition of forskolin and isobutylmethylxanthine. The existence of a cAMP-dependent and a cAMP-independent apoptotic pathway is therefore suggested. Receptor binding studies, RT-PCR experiments and Western blot analysis demonstrated the presence of type 1 kappaor in the CNE2 cells. Stimulation of kappaor in these cells resulted in the production of inositol (1,4,5)-trisphosphate, reduction of cAMP level and a marked enhancement of staurosporine-induced apoptosis. The potentiation of apoptosis by kappaor was prevented by inhibition of phospholipase C but was slightly enhanced by the presence of the active cAMP analogues, 8-CPT-cAMP and dibutyryl-cAMP. These data demonstrate for the first time that the phospholipase C pathway activated by type 1 kappaor expressed by cancer cells is involved in the potentiation of apoptosis. (+info)
Designated organic active ingredient containing (doai) > Heterocyclic carbon compounds containing a hetero ring having...
Plus it
Dezocine - Wikipedia
AID 148750 - Compound was tested for its ability to displace bremazocine from Opioid receptor kappa 2 in hartley guinea pig...
Moxazocine - Wikipedia
TRC | Details of CAS = 1315552-07-8, ChemicalName = N-[(2R,3R,3aS,4S,6aS)-hexahydro-2,4-methano-4H-furo[3,2-b]pyrrol-3-yl...
Tomography | BIII
7,14-Methano-2H,6H-dipyrido[1,2-a:1,2-e][1,5]diazocine, dodecahydro-, [7S-(7α,7aβ,14α,14aβ)]
3aR,4S,7R,7aS) 4,7-Methano-1H-isoindole-1,3(2H)-dione - Manufacturer,Supplier & Exporter
3a,4,5,6,7,7a-hexahydro-4,7-methano-1H-indenyl formate,68683-22-7 - LookChemical.com
1α,3aα,4α,6β,7α,7aα)-octahydro-4,7-methano-1H-... - lll priedas. Inventorius - ECHA
RIFM fragrance ingredient safety assessment 5,8-Methano-2H-1-benzopyran-2-one, 6- ethylideneoctahydro-, CAS Registry Number...
CAS # 33069-62-4, Paclitaxel, 7,11-Methano-5H-cyclodeca[3,4]benz[1,2-b]oxete benzenepropanoic acid deriv., Taxal, Taxol A
PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC | Anesthesiology | ASA Publications
Wound-healing analysis | BIII
octahydro-4,7-methano-1H-indenediyl)bis(methyl... - Registration Dossier - ECHA
Udor KAPPA-43 Complete Diaphragm Kit | J.N. Equipment Superstore
Synthesis and Structure−Activity Relationships of 6,7-Benzomorphan Derivatives as Use-Dependent Sodium Channel Blockers for the...
Plus it
TIMBAL
7759-55-9,98559-77-4,106692-19-7,73037-35-1,5216-82-0,70593-61-2,7065-01-2,37959-19-6,100753-38-6,55566-19-3,
2-Amino-3-phenyl-1-(1-pyrrolidinyl)-1-propanonehydrochloride - Cas No 1236258-19-7 Knowledge - Echemi
Search
Pathology - Grants
- Albert Einstein College of Medicine
December | 2016 | Lysyl hydroxylase signal
Transportation Safety Board of Canada - Aviation Investigation Report A94H0001
Menanggapi Komentar Buruk di Blog | Bibi Titi Teliti
Menanggapi Komentar Buruk di Blog | Bibi Titi Teliti
3-hydroxy-5,5-dimethoxy-3,4-methylenedioxybiphenyl
Summary Report | CureHunter
N-((1-ethyl-5-oxo-2-pyrrolidinyl)methyl)-5-sulfamoyl-2-anisamide
Summary Report | CureHunter
Discovery of a novel selective kappa-opioid receptor agonist using crystal structure-based virtual screening
January | 2014 | microrna inhibitor
Bacterial Respiratory | Adult and Adolescent Opportunistic Infection | AIDSinfo
methyl (2-oxo-3-phenyl-1-pyrrolidinyl)acetate | C13H15NO3 - ChemSynthesis
En iyi biyolojik gübre Üreticilerini ve biyolojik gübre için turkish Konuşan Market Alibaba.comda bulun
CAS # 24622-60-4, 1-(1,3-Benzodioxol-5-yl)-2-(1-pyrrolidinyl)-1-butanone hydrochloride
2-Amino-5-(1-pyrrolidinyl)benzoic acid - Alfa Chemistry
Chemicals and intermediates - China - Trading Company
BIII (Bary x Dantalion Erin II) | Breeding high quality Czechoslovakian Wolfdogs for work and shows.
Plus it
Hexahydro-1,3,5-triethyl-s-triazine supplier distributor- CAS 7779-27-3
EPO - T 0886/91 (Hepatitis B virus/ BIOGEN INC.) of 16.6.1994
Products | Alsachim
Cyclazocine
This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also ... Benzomorphan Archer, S.; Glick, S. D.; Bidlack, J. M. (1996). "Cyclazocine Revisited". Neurochemical Research. 21 (11): 1369- ... novel benzomorphan". J. Pharmacol. Exp. Ther. 302 (1): 374-80. doi:10.1124/jpet.302.1.374. PMID 12065740. S2CID 15864569. ...
Butinazocine
... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan Macdonald F (1997 ...
Anazocine
Benzomorphan F.. Macdonald (1997). Dictionary of Pharmacological Agents. CRC Press. p. 146. ISBN 978-0-412-46630-4. Retrieved ... Anazocine (INN; also known as azabicyclane or CS-307) is an opioid analgesic of the morphan/benzomorphan family developed in ...
Analgesic
Benzomorphans Dezocine. No data available.. Mixed opioid agonist-antagonist.. IM, IV.. Volume of distribution = 9-12 L/kg; half ...
Peripherally acting μ-opioid receptor antagonist
"Antagonist-Agonist Activity of Some N-Substituted Benzomorphans". Advances in Endogenous and Exogenous Opioids. Elsevier: 411- ...
Carbazocine
... is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health Organization ...
Benzazocine
A related compound is benzomorphan. Azocine Benzomorphan v t e. ...
Cogazocine
... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health ...
Phenazocine
... is a much more potent analgesic than pentazocine and other drugs in the benzomorphan series, most probably due to ... It was one of a number of benzomorphan opioids (including pentazocine, dezocine, and cyclazocine) developed in the search for ... Eckenhoff JE (May-June 1959). "Phenazocine, a new benzomorphan narcotic analgesic". Anesthesiology. 20 (3): 355-8. doi:10.1097/ ... "Some Narcotic Antagonists in the Benzomorphan Series". Journal of Pharmacology and Experimental Therapeutics. 143: 141-8. PMID ...
Ketazocine
Benzomorphan Ethylketazocine Leander JD (September 1982). "Effects of ketazocine, ethylketazocine and phenazocine on schedule- ... Ketazocine (INN), also known as ketocyclazocine, is a benzomorphan derivative used in opioid receptor research. Ketocyclazocine ... 1S, 5R, 9R)-2-Cyclopropylmethyl-2'-hydroxy-5, 9-dimethyl-8-oxo-6, 7-benzomorphan hydrochloride monohydrate (ketazocine), ...
Morphan
It is the base of the benzomorphan family of drugs. Benzomorphan Azocine Morphinan Ginsburg, David (1950). "The synthesis of ...
Eptazocine
Benzomorphan Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 396. ISBN 978-3-88763-075-1. ...
Volazocine
... is an opioid analgesic of the benzomorphan class which was never marketed. Benzomorphan ketazocine cyclazocine World ...
Ibazocine
Benzomorphan Dictionary of Pharmacological Agents Volume 2. CRC Press. 21 November 1996. p. 1108. ISBN 978-0-412-46630-4. ...
8-Carboxamidocyclazocine
... novel benzomorphan". The Journal of Pharmacology and Experimental Therapeutics. 302 (1): 374-80. doi:10.1124/jpet.302.1.374. ...
Moxazocine
... (BL-4566) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist ... Reduction of the carbonyl group in oxygenated benzomorphan 1 affords the corresponding alcohol (2). This intermediate is then N ... Cleavage of the phenolic ether by one of the standard schemes affords moxazocine (6). Benzomorphan Dictionary of ...
Gemazocine
... (R-15,497), also known as cyclogemine, is a non-selective opioid antagonist of the benzomorphan class. It may have ... Gelders, Y. G.; de Ranter, C. J.; Schenk, H. (1979). "Structural Studies of Substituted 6,7-Benzomorphan Compounds. I. The ... 7-benzomorphans in the rabbit vas deferens". Eur. J. Pharmacol. 153 (1): 83-7. doi:10.1016/0014-2999(88)90590-0. PMID 2850928. ... Absolute Configuration of (−)-2-Cyclopropylmethyl-2'-hydroxy-5-ethyl-9,9-dimethyl-6,7-benzomorphan (Gemazocine) Hydrobromide". ...
Metazocine
The prototype benzomorphan, metazocine (6), can be obtained from a variation of the morphinan synthesis. Thus, reaction of the ... XI.1Analogs and a Diastereoisomer of 2'-Hydroxy-2,5,9-trimethyl-6,7-benzomorphan". The Journal of Organic Chemistry. 24 (10): ... Further Syntheses in the Benzomorphan Series*1,2". The Journal of Organic Chemistry. 22 (11): 1366-1369. doi:10.1021/ ... Cyclization by means of acid leads directly to the benzomorphan ring system (5). Demethylation of the aromatic ring system ...
Ethylketazocine
Benzomorphan Ketazocine Foye WO, Lemke TL (24 September 2007). Foye's Principles of Medicinal Chemistry. Lippincott Williams & ... Ethylketazocine (WIN-35,197-2), is an opioid drug of the benzomorphan family which has been used extensively in scientific ...
Imine Diels-Alder reaction
7-benzomorphans". J. Heterocycl. Chem. 8 (3): 465. doi:10.1002/jhet.5570080317. Angle, S. R.; Henry, R. M. (1998). "Studies ...
Azocine
Benzomorphan Azocines at the US National Library of Medicine Medical Subject Headings (MeSH). ...
Dezocine
Unlike many other benzomorphans however, it is a silent antagonist of the κ-opioid receptor, and in accordance, does not ... It is related to other benzomorphans such as pentazocine, with a similar profile of effects that include analgesia and euphoria ... Dezocine (INN, USAN) (brand name Dalgan) is a marketed opioid analgesic of the benzomorphan group. First synthesized in 1970, ...
Etazocine
... (NIH-7856) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist ... Benzomorphan National Research Council (U.S.). Committee on Problems of Drug Dependence, American Medical Association. ...
Alazocine
... was one of the early members of the benzomorphan family of opioid analgesics to be investigated. It was first ... The psychotomimetic effects of alazocine and the other benzomorphans were initially attributed incorrectly to agonism of the σ1 ... Subsequently, other benzomorphans, such as pentazocine (an N-dimethylallylbenzomorphan), cyclazocine (an N- ... benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain". Brain Research ...
Proxorphan
Starting material for this preparation is ketoester 1, available by one of the classical benzomorphan syntheses. Condensation ...
Bremazocine
The crystal structure of bremazocine was determined in 1984 Benzomorphan Dortch-Carnes J, Potter DE (2005). "Bremazocine: a ... 7-benzomorphan hydrochloride (bremazocine), C20H29NO2. HCl". Acta Crystallogr. C. 40: 1759-1761. v t e. ...
Quadazocine
... (WIN-44,441) is an opioid antagonist of the benzomorphan family which is used in scientific research. It acts as a ...
Ketorfanol
January 2000). "Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu ...
Benzomorphan - Wikipedia
Benzomorphan | definition of benzomorphan by Medical dictionary
... benzomorphan explanation free. What is benzomorphan? Meaning of benzomorphan medical term. What does benzomorphan mean? ... Looking for online definition of benzomorphan in the Medical Dictionary? ... Benzomorphan , definition of benzomorphan by Medical dictionary https://medical-dictionary.thefreedictionary.com/benzomorphan ... benzomorphan. ben·zo·mor·phan. (benzō-mōrfan), The parent compound of a series of analgesics that includes pentazocine and ...
Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors. - PubMed ...
The benzomorphan compounds displayed a range of affinities in the mu- and delta-opioid receptor expressing cell lines. Good ... Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors.. Abood ME1 ... Displacement assays were performed with eleven (-)-N-alkyl-benzomorphans in the absence and presence of 150 mM NaCl, as well as ... 7-benzomorphans, for which the receptor selectivity and in vivo activity had been characterized recently, and tested them in ...
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in...
PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC | Anesthesiology | ASA Publications
PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC You will receive an email whenever this article is corrected, updated, or ... PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC. Anesthesiology 5 1959, Vol.20, 355-358. doi: ... JAMES E. ECKENHOFF; PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC. Anesthesiology 1959;20(3):355-358. ...
Download Synthetic Analgesics Part Iia Morphinans And Part Iib 67 Benzomorphans 1966
Analgesic - Wikipedia
ATC code N02
Search | The Merck Index Online
Analgesic - New World Encyclopedia
Compound Report Card
Neuropharmacology 2 - Affective disorders and opiates Quiz - By unloopy
Cyclazocine - Wikipedia
This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also ... Benzomorphan Archer, S.; Glick, S. D.; Bidlack, J. M. (1996). "Cyclazocine Revisited". Neurochemical Research. 21 (11): 1369- ... novel benzomorphan". J. Pharmacol. Exp. Ther. 302 (1): 374-80. doi:10.1124/jpet.302.1.374. PMID 12065740. S2CID 15864569. ...
Bupropion Is a Nicotinic Antagonist | Journal of Pharmacology and Experimental Therapeutics
Pentamorphone - The Full Wiki
Hydromorphone
Veit G[au] - PubMed - NCBI
StateMaster - Encyclopedia: Morphine
A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates | PNAS
Patent US5413996 - Targeted drug delivery via phosphonate derivatives - Google Patents
Simple Accordion with CSS & jQuery by Soh Tanaka
Erowid.org: Erowid Reference 1455 : Psychotomimesis mediated by kappa opiate receptors. : Pfeiffer A, Brantl V, Herz A, Emrich...
Plus it
WHOCC - ATC/DDD Index
Popis opojnih droga, psihotropnih tvari i biljaka iz kojih se može dobiti opojna droga te tvari koje se mogu uporabiti za...
Popis opojnih droga, psihotropnih tvari i biljaka iz kojih se može dobiti opojna droga te tvari koje se mogu uporabiti za...
Pentazocine Acetaminophen - FDA prescribing information, side effects and uses
Talacen (Pentazocine and Acetaminophen Tablets): Uses, Dosage, Side Effects, Interactions, Warning
Pentazocine9
- Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma receptors, including the following compounds: 5,9-DEHB 8-CAC Alazocine Anazocine Bremazocine Butinazocine Carbazocine Cogazocine Cyclazocine Dezocine Eptazocine Etazocine Ethylketocyclazocine Fluorophen Gemazocine Ibazocine Ketazocine Metazocine Moxazocine Pentazocine Phenazocine Quadazocine Thiazocine Tonazocine Volazocine Zenazocine Some of these agents are used as analgesics, including pentazocine, phenazocine, dezocine, and eptazocine. (wikipedia.org)
- INTRODUCTION: Pentazocine, belonging to benzomorphan series was the first mixed agonist-antagonist opioid analgesic to be marketed. (thefreedictionary.com)
- Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). (drugs.com)
- Pentazocine, an opioid benzomorphan derivative which causes analgesia, respiratory depression, and sedation similar to other opioids. (mims.com)
- Sigma-1 receptor ligands include cocaine, (+)-benzomorphans like (+)-pentazocine and (+)N-allyl-normetazocine (or (+)- SKF-10047), and endogenous neurosteroids like progesterone and pregnenolone sulfate. (ingentaconnect.com)
- It's funny, this pentazocine - it's classified as a benzomorphan (what an interesting name) or benzazocine. (sixthseal.com)
- Pentazocine: This benzomorphan derivative is a lack of precise control and the area result in accidental vascular injury bleeding need for surgery the patient should be performed to anastomose right hemivagina and ipsilateral fallopian tube is elevated if it were the most severe form of strabismus characterized by heightened sympathetic activity. (bigsurlandtrust.org)
- Pregnant women may desire contraception immediately after surgery society recommendations have not received the earlier stage i.E, pentazocine: This benzomorphan derivative is a communicating vessel between the ages of children. (yogachicago.com)
- Synthetic opioids are structurally distinct chemical products obtained in order to bind to the opioid receptors, and are also sub-classified according to the chemical structure into phenylpyperidines (pethidine, fentanyl), diphenylpropalamines (methadone), morphinans (levorphanol) and benzomorphans (pentazocine). (uop.edu.jo)
Derivatives1
- The trivalent compounds and congeners, e.G., levorphanol and p bestil viagra nettet butorphanol iv benzomorphan derivatives, e.G., tolazoline and phentolamine, cause competitive non-selective adrenergic blockade. (cadasb.org)
Morphinans1
- download synthetic analgesics part iia morphinans and part iib 67 benzomorphans 1966 being relates from density who would navigate including it convincing via a coming meeting like Twitch. (cityslide.de)
Opioid6
- Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors. (nih.gov)
- To evaluate the potential of this system, we chose a series of (-)-5,9 alpha-dimethyl-2-hydroxy-N-substituted-6,7-benzomorphans, for which the receptor selectivity and in vivo activity had been characterized recently, and tested them in CHO cells stably transfected with either the rat delta-opioid receptor or the mouse mu-opioid receptor. (nih.gov)
- The benzomorphan compounds displayed a range of affinities in the mu- and delta-opioid receptor expressing cell lines. (nih.gov)
- This family of opioid drugs is called the benzomorphans or benzazocines. (wikipedia.org)
- 2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist. (bioportfolio.com)
- First described by Martin and his colleagues (1976) to account for the behavioral effects of selected benzomorphan opiates, sigma binding sites were originally classified as an opioid receptor subtype. (springer.com)
Opiates2
- Specific [ 3 H]phencyclidine binding can be displaced by cyclazocine (IC 50 = 350 nM) and by related benzomorphans, but not by classical opiates such as morphine or naloxone. (elsevier.com)
- The authors thus propose a common binding site in rat nervous tissue for phencyclidine and some of the benzomorphan opiates. (elsevier.com)
Morphine1
- The 4-(m-OH-phenyl)piperidines are a flexible fragment of the morphine/benzomorphan fused-ring opioids. (aspetjournals.org)
Agonist3
- This synthetic member of the benzomorphan series is structurally similar to other drugs having the various degrees of narcotic agonist and antagonist properties at room temperature. (thefreedictionary.com)
- The benzomorphan kappa agonist MR 2033 is inactive at sigma-phencyclidine receptors. (erowid.org)
- Other drugs that produced discriminative effects similar to those of EKC were the narcotic agonists, ketazocine and UM 909 (an N-methylfuryl substituted benzomorphan), and the mixed agonist-antagonists, cyclazocine, cyclorphan, SKF-10,047 (N-allylnormetazocine) and nalorphine. (ttu.edu)
Affinity1
- The σ 2 receptor was initially identified by radioligand-binding studies as a binding site with high affinity for di- o -tolylguanidine (DTG) ( K i = 21.2 nM) and haloperidol ( K i = 48.7 nM) ( 3 ) but with low affinity for (+)-benzomorphans ( 9 ). (pnas.org)
Cocaine1
- subsequent studies showed that the σ receptors were able to bind a variety of pharmacologically effective drugs, including benzomorphans, neuroleptics, antidepressants, cocaine, peptides related to neuropeptide Y, and neurosteroids (for review, see ref. 3 ), although intriguingly no known natural specific ligand(s) have been discovered. (aacrjournals.org)
Compounds1
- These are aromatic compounds containing a 6,7-benzomorphan skeleton, which is substituted by methyl group at the 2- and 6-positions. (wishartlab.com)
Selective2
- Displacement assays were performed with eleven (-)-N-alkyl-benzomorphans in the absence and presence of 150 mM NaCl, as well as known delta- and mu-selective agonists. (nih.gov)
- Cells selective for benzomorphan drugs. (haverford.edu)
Pharmacological1
- The pivotal role of the stereocenter at the N-substituent of the 6,7-benzomorphan scaffold was investigated combining synthetic and pharmacological approaches. (bioportfolio.com)
Vivo1
- Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties. (sigmaaldrich.com)