Dezocine

Dezocine Basic information
Product Name:Dezocine
Synonyms:dezocine;[5R-(5α,11α,13S^<*>^)]-13-Amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,1 1-metha-nobenzocyclodecen-3-ol;Dalgan;Wy-16225;Wy-16225V;(13S)-13-Amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5α,11α-methanobenzocyclodecen-3-ol;13-Amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,11-methanobenzocyclodecen-3-ol;(5R,11S,13S)-13-AMino-5-Methyl-5,6,7,8,9,10,11,12-octahydro-5,11-Methanobenzo[10]annulen-3-ol
CAS:53648-55-8
MF:C16H23NO
MW:245.36
EINECS:
Product Categories:Amines;Aromatics;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals
Mol File:53648-55-8.mol
Dezocine Structure
Dezocine Chemical Properties
Melting point >124°C (dec.)
Boiling point 392.6±42.0 °C(Predicted)
density 1.082±0.06 g/cm3(Predicted)
storage temp. Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility DMSO (Slightly), Methanol (Slightly)
pka10.06±0.40(Predicted)
form Solid
color White to Off-White
Safety Information
RIDADR 3249
HazardClass 6.1(b)
PackingGroup III
MSDS Information
Dezocine Usage And Synthesis
DescriptionDezocine is an injectable agonisthtagonist analgesic indicated when an opioid analgesic is suitable for the management of pain. The drug differs from other opioid agonisthtagonists by having a high affinity for both the mu and delta receptors and a low effect on kappa receptors. Dezocine is reported to have a rapid onset of action, short half-life and low abuse potential with insignificant side effects.
OriginatorWyeth-Ayerst (American Home Products) (U.S.A.)
UsesDezocine is an opioid analgesic that is related to Pentazocine (P274300). Dezocine is used to relieve post-operative pain with its potency comparable to Meperidine (M223900).
DefinitionChEBI: (7S,8S)-7-Amino-8-methyl-5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogen at position 8 and one of the hydrogens at position 6 are substituted by each end of a tetramethylene bridge. A synthetic opioid analgesic, it has mixed opiod agonist and antagonist properties. Although it is used for pain management, it can produce opioid withdrawal syndrome in patients already dependent on other opioids, and its clinical application is limited by side effects such as dizziness.
Brand nameDalgan (AstraZeneca).
Biological FunctionsDezocine (Dalgan) is a synthetic aminotetralin derivative with potent agonist–antagonist effects.The onset of activity and potency as an analgesic are comparable to those of morphine. Although the drug requires glucuronidation during metabolism, patients with hepatic insufficiency clear it normally.The main route for clearance is the kidney.Thus, patients with renal dysfunction are prone to buildup of dezocine over time. As an antagonist, dezocine is more potent than pentazocine. As an agonist, dezocine produces analgesia and respiratory depression (which is readily reversed by naloxone), but unlike pentazocine, it has little if any effect on the cardiovascular system.
Dezocine is indicated as an analgesic for moderate to severe pain. In addition, it shows promise in chronic pain states, such as with victims of severe burns. Contraindications and adverse effects of the drug are similar to those described for morphine. No tendency toward abuse has been demonstrated thus far.
Mechanism of actionDezocine is classified as a mixed agonist/antagonist. The SAR of dezocine is unique among the opioids. It is a primary amine, whereas all other nonpeptide opioids are tertiary amines. Its exact receptor selectivity profile has not been reported; however, its pharmacology is most similar to that of buprenorphine. It seems to be a partial agonist at μ receptors, to have little effect at κ receptors, and to exert some agonist effect at δ receptors.
Clinical UseIt is useful for the treatment of moderate to severe pain. It is available for intramuscular and intravenous dose. The drug is indicated for postoperative and cancerinduced pain.
Dezocine Preparation Products And Raw materials
Raw materialsActivated carbon,decolor
Methylparaben Methyl Methyl cyclopentenolone Bensulfuron methyl 1,1,3-TRIMETHYLTETRALIN Parathion-methyl (R)-4-(3-AMINO-BUTYL)-PHENOL Norandrostenedione Dezocine Kresoxim-methyl Allyl methacrylate Thiophanate-methyl 7-AMINO-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-OL EPTAZOCINE Methyl acrylate Methyl bromide N,N-Dimethyl-1,4-phenylenediamine METHYL THIOPHENE-2-CARBOXYLATE

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