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Benzomorphan
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. See also * Benzazocine * Azocine * Morphinan Morphinan is the prototype chemical structure of a large chemical class of psychoactive drugs, consisting of opiate analgesics, cough suppressants, and dissociative hallucinogens, among others. Structure Morphinan has a phenanthrene core stru ... References Benzomorphans {{organic-compou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etazocine
Etazocine (NIH-7856) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist of the opioid receptors, with mixed agonist and receptor antagonist, antagonist effects. In animal studies, it was shown to induce analgesia, physical dependence, dependency, and respiratory depression, with overall effects similar to those of morphine, but with substantially reduced potency (pharmacology), potency in comparison. See also * Benzomorphan References {{Opioidergics Phenols Analgesics Benzomorphans Opioids ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Butinazocine
Butinazocine (INN) is an opioid analgesic of the benzomorphan family which was never marketed. See also * Benzomorphan 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 ... References {{Opioidergics Analgesics Benzomorphans Opioids ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibazocine
Ibazocine (INN, USAN) is an opioid analgesic which was never marketed. See also * Benzomorphan 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 ... References Analgesics Benzomorphans Opioids {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketazocine
Ketazocine (INN), also known as ketocyclazocine, is a benzomorphan derivative used in opioid receptor research. Ketazocine, for which the receptor is named, is an exogenous opioid that binds to the κ opioid receptor. Activation of this receptor is known to cause sleepiness, a decrease in pain sensation and (potentially) dysphoria, paranoia, and hallucinations. It also causes an increase in urine production because it inhibits the release of vasopressin. (Vasopressin is an endogenous substance that assists in regulating fluid and electrolyte balance in the body and decreases the amount of water released into the urine.) Unlike other opioids, substances that only bind to the κ receptor theoretically do not depress the respiratory system. The crystal structure of ketazocine was determined in 1983. See also * Benzomorphan 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 follow ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metazocine
Metazocine is an opioid analgesic related to pentazocine. While metazocine has significant analgesic effects, mediated through a mixed agonist–antagonist action at the mu opioid receptor, its clinical use is limited by dysphoric and hallucinogenic effects which are most likely caused by activity at kappa opioid receptors (where it is a high-efficacy agonist) and/or sigma receptors. Metazocine is in Schedule II of the Controlled Substances Act 1970 of the United States as a Narcotic with ACSCN 9240 with a 19 gram aggregate manufacturing quota as of 2014. The free base conversion ratio for salts includes 0.81 for the hydrochloride and 0.74 for the hydrobromide. It is listed under the Single Convention for the Control of Narcotic Substances 1961 and is controlled in most countries in the same fashion as is morphine. Syntheses The prototype benzomorphan, metazocine (6), can be obtained from a variation of the morphinan synthesis. Thus, reaction of the Grignard reagent from ''p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclazocine
Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also has high affinity for the DOR. Use Research into the use of cyclazocine for the treatment of bipolar patients with depression was undertaken by Fink and colleagues (1970). It showed that 8 out of 10 patients experienced moderate improvement. Research during the 1960s and 1970s into the possible use of cyclazocine for management of pain, and later for assisting treatment of narcotic addiction was severely hampered by the drug's psychotomimetic, dysphoric, and hallucinatory effects. The dysphoric/ anxiety inducing effects of the drug correlate with increasing dosage and would likely reduce the risk of abuse in the same manner as other opioids which preferentially act on the KOR versus the DOR and MOR, although the side-effect threshold is often lower ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cogazocine
Cogazocine (INN) is an opioid analgesic of the benzomorphan family which was never marketed. See also * Benzomorphan 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 ... References {{Opioidergics Phenols Analgesics Benzomorphans Opioids Cyclobutyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Moxazocine
Moxazocine (BL-4566) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist or mixed agonist/antagonist of the opioid receptors and binds preferentially to the κ-opioid receptor. Despite its failure to reach the market, clinical studies demonstrated moxazocine to be approximately 10x as potent by weight as morphine as an analgesic. Synthesis Reduction of the carbonyl group in oxygenated benzomorphan 1 affords the corresponding alcohol (2). This intermediate is then N-demethylated by means of BrCN. Acylation with cyclopropylcarbonyl chloride gives the amide (3). The alcohol is then converted to the ether by treatment with MeI and base (4). Treatment with LiAlH4 serves to reduce the amide function. Cleavage of the phenolic ether by one of the standard schemes affords moxazocine (6). See also * Benzomorphan Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bremazocine
Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic effects. It has 200 times the activity of morphine, but appears to have no addictive properties and does not depress breathing. The crystal structure of bremazocine was determined in 1984 See also * Benzomorphan 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 * Butinazoc ... References Synthetic opioids Phenols Benzomorphans Kappa-opioid receptor agonists Tertiary alcohols Cyclopropanes {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gemazocine
Gemazocine (R-15,497), also known as cyclogemine, is a non-selective opioid antagonist of the benzomorphan class. It may have partial agonist properties at some of the opioid receptor Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin ...s, such as at the kappa receptor (as it induces dysphoric effects in humans), but seems to be generally antagonistic in its actions. References Benzomorphans Kappa-opioid receptor agonists Mu-opioid receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenazocine
Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects. Effects of phenazocine include analgesia and euphoria, also may include dysphoria and hallucinations at high doses, most likely due to action at κ-opioid and σ receptors. Phenazocine appears to be a much stronger analgesic with fewer side effects than pentazocine, probably due to a more favorable μ/κ binding ratio. Phenazocine is a much more potent analgesic than pentazocine and other drugs in the benzomorphan series, most probably due to the presence of an ''N''-phenethyl substitution, which is known to boost μ-opioid activity in many classes of opioid analgesics. Also, it does not cause spasm of the sphincter of Oddi, making it more suitable than morphine for the treatment of biliary or pancreatic pain. Regarding the two enantiomers of phenazocine, (''R'')-phenazocine has twenty times the potency of morphine as an analgesic, wh ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Volazocine
Volazocine is an opioid analgesic of the benzomorphan class which was never marketed. Synthesis See also * Benzomorphan *ketazocine *cyclazocine Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also has high affinit ... References Analgesics Benzomorphans Opioids {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
