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Gemazocine

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Gemazocine
Clinical data
ATC code
  • None
Identifiers
  • 10-(cyclopropylmethyl)-1-ethyl-13,13-dimethyl-10-azatricyclo[7.3.1.02,7]trideca-2,4,6-trien-4-ol
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC20H29NO
Molar mass299.458 g·mol−1
3D model (JSmol)
  • Oc1ccc4c(c1)C2(C(C(N(CC2)CC3CC3)C4)(C)C)CC
  • InChI=1S/C20H29NO/c1-4-20-9-10-21(13-14-5-6-14)18(19(20,2)3)11-15-7-8-16(22)12-17(15)20/h7-8,12,14,18,22H,4-6,9-11,13H2,1-3H3
  • Key:AFZOCGNTFCGOEE-UHFFFAOYSA-N

Gemazocine (R-15,497), also known ascyclogemine, is a non-selectiveopioid antagonist of thebenzomorphan class.[1][2][3] It may havepartial agonist properties at some of theopioid receptors, such as at the kappa receptor (as it induces dysphoric effects in humans), but seems to be generallyantagonistic in its actions.[4]

References

[edit]
  1. ^Macdonald F (1997).Dictionary of Pharmacological Agents. CRC Press. p. 955.ISBN 978-0-412-46630-4. Retrieved22 April 2012.
  2. ^Gelders YG, de Ranter CJ, Schenk H (1979)."Structural Studies of Substituted 6,7-Benzomorphan Compounds. I. The Absolute Configuration of (−)-2-Cyclopropylmethyl-2'-hydroxy-5-ethyl-9,9-dimethyl-6,7-benzomorphan (Gemazocine) Hydrobromide".Acta Crystallographica B.35 (3):699–703.Bibcode:1979AcCrB..35..699G.doi:10.1107/S0567740879004477.
  3. ^Verlinde C, De Ranter C (August 1988). "Assessment of the kappa-opioid activity of a series of 6,7-benzomorphans in the rabbit vas deferens".European Journal of Pharmacology.153 (1):83–87.doi:10.1016/0014-2999(88)90590-0.PMID 2850928.
  4. ^Freye E, Hartung E, Schenk GK (May 1983)."Bremazocine: an opiate that induces sedation and analgesia without respiratory depression".Anesthesia and Analgesia.62 (5):483–488.doi:10.1213/00000539-198305000-00005.PMID 6301311.
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others
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