Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 15, 1997, Pages 1963-1968

  Olesen, P H ^a   Swedberg, M D B ^a   Eskesen, K ^a   Judge, M E ^a   Egebjerg, J ^a   Tonder J E ^a   Rasmussen, T ^a   Sheardown, M J ^a   Rimvall, K ^a  

^a NOVO NORDISK A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

3 (5 METHYL 3 ISOXAZOLYL)METHYLENE 1 AZABICYLO[2.2.2]OCTANE; 3 METHYL 5 (1 METHYL 2 PYRROLIDINYL)ISOXAZOLE; METHYLCARBACHOL; MUSCARINIC RECEPTOR; NICOTINE; NICOTINIC AGENT; NICOTINIC RECEPTOR; OXOTREMORINE; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BIOAVAILABILITY; BRAIN CORTEX; CELL LINE; CONTROLLED STUDY; CORPUS STRIATUM; DOPAMINE RELEASE; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; ENANTIOMER; HUMAN; IN VITRO STUDY; INSECT; LOCOMOTION; NONHUMAN; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; OOCYTE; ORAL DRUG ADMINISTRATION; PROTEIN EXPRESSION; RAT; SUBCUTANEOUS DRUG ADMINISTRATION; XENOPUS;

EID: 0030806755     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00347-8     Document Type: Article

References (19)

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16. 2+. Superfusion of agonist and sampling of current responses measured with the oocytes voltage clamped at -60 mV were all controlled by a customized program. The data are expressed as percentage of current response induced by 1 μM and 30 μM nicotine for the α4β2 and the α3β2 subtype, respectively.
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19. Mice were injected subcutaneously with the test compounds 30 min prior to testing. Testing occurred in sound isolated photo cell activity boxes. Animals were tested individually for 10 min.