Morphine derivatives of the methanobenzazocine family that act as potent analgesics.
A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.
Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.
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.

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)

Benzomorphans are a class of synthetic opioid analgesics that are structurally related to the benzomorphan natural product codeine. They are characterized by the presence of a benzene ring attached to a morphinan skeleton, which is a six-membered ring containing an oxygen atom and a nitrogen atom. Benzomorphans are used as painkillers and have been found to be effective in managing moderate to severe pain. However, they are also highly addictive and can cause respiratory depression, which can be life-threatening. As a result, benzomorphans are controlled substances and are only available by prescription from a healthcare provider. Some examples of benzomorphans include pentazocine, butorphanol, and nalbuphine. These drugs are often used in combination with other painkillers, such as acetaminophen or nonsteroidal anti-inflammatory drugs (NSAIDs), to provide more effective pain relief.

Levorphanol is a synthetic opioid analgesic medication that is used to relieve moderate to severe pain. It is a derivative of the opiate morphine and is similar in structure to other opioids such as oxycodone and hydrocodone. Levorphanol is available in both oral and injectable forms and is often used in hospitals and other medical settings to manage pain in patients who are recovering from surgery or who have chronic pain conditions. It is a Schedule II controlled substance in the United States, which means that it has a high potential for abuse and dependence. Like other opioids, levorphanol can cause side effects such as drowsiness, nausea, constipation, and respiratory depression. It is important to use levorphanol only under the guidance of a healthcare professional and to follow their instructions carefully to minimize the risk of adverse effects.

Morphinans are a class of drugs that are derived from the opium poppy and are used to relieve pain. They work by binding to specific receptors in the brain and spinal cord, known as mu-opioid receptors, which are involved in the body's response to pain. Morphinans are used to treat a wide range of painful conditions, including acute pain, chronic pain, and cancer pain. They are available in various forms, including tablets, capsules, injections, and transdermal patches. However, they can also be addictive and can cause side effects such as nausea, vomiting, constipation, dizziness, and respiratory depression.

Receptors, sigma (σ receptors) are a type of G protein-coupled receptors (GPCRs) that are found in the central nervous system and other tissues. They are activated by a variety of endogenous and exogenous ligands, including certain drugs and neurotransmitters. σ receptors are thought to play a role in a number of physiological processes, including pain perception, mood regulation, and the regulation of stress responses. They are also believed to be involved in the development of certain neurological disorders, such as schizophrenia and addiction. There are two main subtypes of σ receptors: σ1 receptors and σ2 receptors. σ1 receptors are found primarily in the brain and are thought to play a role in modulating the effects of other neurotransmitters, such as dopamine and serotonin. σ2 receptors are found throughout the body and are thought to play a role in regulating cell growth and survival. In the medical field, σ receptors are being studied as potential targets for the development of new drugs for the treatment of a variety of conditions, including pain, anxiety, and addiction.

... is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma ... Benzomorphans, All stub articles, Organic compound stubs). ...
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. ...
... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan Macdonald F (1997 ...
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 ...
"Antagonist-Agonist Activity of Some N-Substituted Benzomorphans". Advances in Endogenous and Exogenous Opioids. Elsevier: 411- ...
... is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health Organization ...
A related compound is benzomorphan. Azocine Benzomorphan v t e (Articles without EBI source, Articles without KEGG source, ...
... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health ...
... 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/ ... Benzomorphans, Kappa-opioid receptor agonists, Mu-opioid receptor agonists, Phenols, Synthetic opioids). ...
Benzomorphan Ethylketazocine Leander JD (September 1982). "Effects of ketazocine, ethylketazocine and phenazocine on schedule- ... Verlinde CL, De Ranter CJ (1983). "(1S, 5R, 9R)-2-Cyclopropylmethyl-2'-hydroxy-5, 9-dimethyl-8-oxo-6, 7-benzomorphan ... Ketazocine (INN), also known as ketocyclazocine, is a benzomorphan derivative used in opioid receptor research. Ketazocine, for ... Benzomorphans, Kappa-opioid receptor agonists, Ketones, Phenols, Synthetic opioids). ...
It is the base of the benzomorphan family of drugs. Benzomorphan Azocine Morphinan Ginsburg, David (1950). "The synthesis of ...
Benzomorphan Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 396. ISBN 978-3-88763-075-1. ...
... is an opioid analgesic of the benzomorphan class which was never marketed. Benzomorphan ketazocine cyclazocine World ... Benzomorphans, Opioids, All stub articles, Analgesic stubs). ...
... novel benzomorphan". The Journal of Pharmacology and Experimental Therapeutics. 302 (1): 374-80. doi:10.1124/jpet.302.1.374. ... Benzomorphans, Kappa-opioid receptor agonists, Mu-opioid receptor agonists, Carboxamides). ...
... (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 ...
Verlinde C, De Ranter C (August 1988). "Assessment of the kappa-opioid activity of a series of 6,7-benzomorphans in the rabbit ... 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 ... Benzomorphans, Kappa-opioid receptor agonists, Mu-opioid receptor antagonists, All stub articles, Nervous system drug stubs). ...
Benzomorphan Ganellin CR, Triggle DJ (21 November 1996). Dictionary of Pharmacological Agents Volume 2. CRC Press. p. 1108. ... Benzomorphans, Opioids, All stub articles, Analgesic stubs). ...
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 ...
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 ...
7-benzomorphans". J. Heterocycl. Chem. 8 (3): 465. doi:10.1002/jhet.5570080317. Angle, S. R.; Henry, R. M. (1998). "Studies ...
... has a structure similar to the benzomorphan group of opioids. Dezocine is unusual among opioids as it is one of the ...
... (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. ...
... 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 ...
Starting material for this preparation is ketoester 1, available by one of the classical benzomorphan syntheses. Condensation ... Benzomorphans, Kappa-opioid receptor agonists, Opioids, Phenols, All stub articles, Analgesic stubs). ...
The crystal structure of bremazocine was determined in 1984 Benzomorphan Dortch-Carnes J, Potter DE (2005). "Bremazocine: a ... Benzomorphans, Kappa-opioid receptor agonists, Tertiary alcohols, Cyclopropanes, All stub articles, Analgesic stubs). ... 7-benzomorphan hydrochloride (bremazocine), C20H29NO2. HCl". Acta Crystallogr. C. 40 (10): 1759-1761. doi:10.1107/ ...
... (WIN-44,441) is an opioid antagonist of the benzomorphan family which is used in scientific research. It acts as a ... Benzomorphans, Cyclopentyl compounds, Delta-opioid receptor antagonists, Kappa-opioid receptor antagonists, Mu-opioid receptor ...
January 2000). "Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu ...
Chemically it is classed as a benzomorphan and it comes in two enantiomers, which are molecules that are exact (non- ... Benzomorphans, Kappa-opioid receptor agonists, Phenols, Sigma agonists, Synthetic opioids). ...
US 4406904, Welle HB, Marko M, "Method of inhibiting luteinizing hormone secretion with 6,7-benzomorphan derivatives", issued ...
... benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain". Brain Res. 527 ...
2-hydroxy-5,9-dimethyl-2-phenethyl-6,7-benzomorphan. Phenomorphan. 3-hydroxy-N-phenethylmorphinan ...
7-benzomorphan]. The release of norepinephrine evoked by 5 Hz of ES was inhibited by DAMGO (10(-10) to 10(-6) M), but not by U- ...
Effects of the psychotomimetic benzomorphan N-allylnormetazocine (SKF 10,047) on prepulse inhibition of startle in mice. ... N-allylnormetazocine (NANM; SKF 10,047) is a benzomorphan opioid that produces psychotomimetic effects. (+)-NANM is the ... and there is a widespread belief that the hallucinogenic effects of NANM and other benzomorphan derivatives are mediated by ...
These results show that the benzomorphan MR-2034 stimulates the HPA axis in the rat by acting at the hypothalamic and the ... These results show that the benzomorphan MR-2034 stimulates the HPA axis in the rat by acting at the hypothalamic and the ...
Benzomorphans / pharmacology Actions. * Search in PubMed * Search in MeSH * Add to Search ...
Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). Chemically, pentazocine is (2R*,6R*, ...
Based on Mays work on benzomorphans, the drug pentazocine was introduced in the 1960s. Pentazocine was the first drug used in ...
Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.. Carroll FI; Bai ...
Benzomorphans,N0000007550, Phenyl Ethers,N0000007549, Benzofurans,N0000007548, Benzodiazepinones,N0000007547, Phenoxyacetates, ...
Benzomorphan Narrower Concept UI. M0002364. Registry Number. 0. Terms. Benzomorphan Preferred Term Term UI T004565. Date04/16/ ... Benzomorphan Registry Number. 0. Public MeSH Note. 91; was see under MORPHINANS 1985-90; was BENZOMORPHAN see under MORPHINANS ... use BENZOMORPHANS to search BENZOMORPHAN 1975-84; use MORPHINANS 1973-74 & BRIDGED COMPOUNDS 1966-72. History Note. 91(85); was ... Benzomorphans Preferred Term Term UI T004564. Date01/01/1999. LexicalTag NON. ThesaurusID NLM (1975). ...
Benzomorphan Narrower Concept UI. M0002364. Registry Number. 0. Terms. Benzomorphan Preferred Term Term UI T004565. Date04/16/ ... Benzomorphan Registry Number. 0. Public MeSH Note. 91; was see under MORPHINANS 1985-90; was BENZOMORPHAN see under MORPHINANS ... use BENZOMORPHANS to search BENZOMORPHAN 1975-84; use MORPHINANS 1973-74 & BRIDGED COMPOUNDS 1966-72. History Note. 91(85); was ... Benzomorphans Preferred Term Term UI T004564. Date01/01/1999. LexicalTag NON. ThesaurusID NLM (1975). ...
use BENZOMORPHANS to search BENZOMORPHAN 1975-84; use MORPHINANS 1973-74 & BRIDGED COMPOUNDS 1966-72. ... Benzomorphans - Preferred Concept UI. M0002363. Scope note. Morphine derivatives of the methanobenzazocine family that act as ... 91(85); was see under MORPHINANS 1985-90; was BENZOMORPHAN see under MORPHINANS 1973-84 & see under BRIDGED COMPOUNDS 1966-72. ... 91; was see under MORPHINANS 1985-90; was BENZOMORPHAN see under MORPHINANS 1973-84 & see under BRIDGED COMPOUNDS 1966-72. ...
2-hydroxy-2,5,9-trimethyl-6,7-benzomorphan. Methadone (metadon). 6-dimethylamino-4,4-diphenyl-3-heptanone. ...
Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). Chemically, pentazocine lactate is 6 ... Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). ...
Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). Chemically, pentazocine ...
7-benzomorphans (e.g. metazocine). Although seemingly structurally diverse, all these compounds either possess a piperidine ...
... drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain. Pentazocine is sold under several ...
D2.455.426.559.847.181 Benzomorphans D3.132.610.422.106 D3.132.577.249.106 D4.615.723.795.106 Benzopyrenes D2.455.426.559. ...
Benzomorphans 142 Phenolic hydroxyl in a- and ^-benzomorphans. 143 /3-benzomorphans, more potent series 143 Codeinone series ...
7-benzomorphans, in that they have an equatorially oriented aromatic ring rather than the axial orientation of that ring found ...
Benzomorphans Benzophenanthridines Benzophenoneidum Benzophenones Benzopyrans Benzopyrene Hydroxylase Benzopyrenes TERM ...
  • Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic (opioid analgesic) drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain. (ncats.io)
  • Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). (nih.gov)
  • Based on May's work on benzomorphans, the drug pentazocine was introduced in the 1960s. (nih.gov)