Alazocine

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Alazocine
Alazocine.svg
Clinical data
Routes of
administration
?
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEMBL
ECHA InfoCard 100.162.264
Chemical and physical data
Formula C17H23NO
Molar mass 257.37 g/mol
3D model (Jmol)
 NYesY (what is this?)  (verify)

Alazocine ((-)-SKF-10,047), or (-)-N-allylnormetazocine ((-)-ANMC), was the first drug discovered to act as a σ1 receptor agonist (Ki = 24 nM).[1][2][3] It has no significant affinity for the σ2 receptor.[3] Alazocine also acts as a κ-opioid receptor partial agonist (Ki = 0.4 nM; EC50 = 24 nM; Emax = 66%),[4] and to a much lesser extent, as an NMDA receptor antagonist (Ki = 587 nM).[3][5]

See also[edit]

References[edit]

  1. ^ Iwamoto ET (February 1981). "Pharmacologic effects of N-allylnormetazocine (SKF-10047)". NIDA Research Monograph. 34: 82–8. PMID 6783955. 
  2. ^ Shearman GT, Herz A (August 1982). "Non-opioid psychotomimetic-like discriminative stimulus properties of N-allylnormetazocine (SKF 10,047) in the rat". European Journal of Pharmacology. 82 (3–4): 167–72. PMID 6290235. doi:10.1016/0014-2999(82)90506-4. 
  3. ^ a b c Chou YC, Liao JF, Chang WY, Lin MF, Chen CF (March 1999). "Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan". Brain Research. 821 (2): 516–9. PMID 10064839. doi:10.1016/S0006-8993(99)01125-7. 
  4. ^ Gharagozlou, Parham; Hashemi, Ezzat; DeLorey, TimothyM; Clark, J David; Lameh, Jelveh (2006). "Pharmacological profiles of opioid ligands at Kappa opioid receptors". BMC Pharmacology. 6 (1): 3. ISSN 1471-2210. PMC 1403760Freely accessible. PMID 16433932. doi:10.1186/1471-2210-6-3. 
  5. ^ Gharagozlou P, Hashemi E, DeLorey TM, Clark JD, Lameh J (2006). "Pharmacological profiles of opioid ligands at Kappa opioid receptors". BMC Pharmacology. 6 (1): 3. PMC 1403760Freely accessible. PMID 16433932. doi:10.1186/1471-2210-6-3.