Interaction of Tacrine at M1 and M2 Cholinoceptors in Guinea Pig Brain

Maria Szilagyi, Wai-Man Lau
1993 Pharmacology  
EllIilhlll AGE I AGENCY USE ONLY 2 REPORT DATE 3 "YPE.•DTES COVEED I19W3 4 -E AND Interaction of Tacrine at M1 and M2 5 FUNDING NUMBERS cholinoceptors in Guinea Pig Brain 6 AUTHOR Maria Szilagyi and Wai-Man Lau 7 FOAMING ORG KES/eADORENESS DEFENCE SCIENCE AND S PEFORMING Wa REPO" NO TECHNOLOGY ORGANIZATION, MATERIALS RESEARCH LABORATORY, PO BOX 50, ASCOT VALE VICTORIA 3032 AUSTRALIA oS SPONISORINQIMONITUNG AGENCY NAMES AND AODRESSES 1 ISUPPLEMENTARY NOTES 12 DISTRIBUTION/AVAILABIuIY STATEMENT
more » ... LABIuIY STATEMENT 12B DoSTIBUTION CODE DISTRIBUTION STATEMENT A 1 13. ABSTRACT (MAX 200 WORM): Tacrin (THA) selecvly fmoduldse binding of M1 NIw m in an alloesc fmhion coming posi0ve coopersvly. The nOhild of -TA to MI md M2 cholnoepinom i emimw. ft tieeforew d poposed OW the I'me-c seleadvity of THA is a kwmdon of tue Ibin aft aid not of THA iell. It inter.ailon of MI and M2 cho•nocepbir wa exanined in guinea pig brain homogenrulus tuO eelho•ve M1 eid M2 mtionlamW(3H)-p inMeine ((3,))PZ) ad (3H)AF-OX 364. The dseackdionCotn. were 0.36 nmolW for Vte MI rmepior mid 0.23nmolI for to M2 recepitr. Weslooompw'ed tuebinding ofTHAmid meltuocrmine (MTA) sM2 ,ecepbiaiece 14 SUBJECT TERMS 15 NUMBER OF PAGES 6 16 PRICE CODE Abstract Tacrine Tacrine (TI-A) selectively modulates binding of M 1 ligands in Cholinoceptors, M, and M 2 an allosteric fashion causing positive cooperativity. The binding affinity of THA to M 1 and M 2 cholinoceptors is similar. It is therefore proposed that the allosteric selectivity of THA is a function of the binding site and not of THA itself. Its interaction of M I and M 2 cholinoceptors was examined in guinea pig t brain homogenates using the selective M, and M 2 antagonists
doi:10.1159/000139101 pmid:8234410 fatcat:rs5w4ypxarfmnhp4kd3xm5mqei