To: John H Rcynolds Dalc: Scplember 2 1986 From: RM Lippicllo Subject: Highlights Tcsting ol polentia! ncw ligands for nicoline reccplor binding N-melhyl cylisice studics conlinucd: inas yithesizcd by _D5: Toras Hudlicky (VFI) anc forarded t0 RJR for asscssmcn ot Ils potzngy in inhibition binding assay3 This compound was found to be approximately 100-fold less elicctivc in inhibiting (3HJ-nicotine binding (0 rat brain tissue than its parent compound, cylisinc, and 1S-told Iess potent than dolng L-Eolinc in the N-mcthyl derivalive docs nOt appcar (8 be suitable a5 Thcrcforc, potcntia) ndioligard for nicotine reccpto; characterization: Thc synthcsis of halogenated derivatives 0l Gylisine will now be undcrtakcn: 2 Repurification o L[3H] nicotinc, routinely utilized in nicoline receplor studics, bcamc ncccssary because ound that commercially available material containcd 13-18 % radiochcmicl impuritics. Rias Recent cvidence in the literaturc, based model ccll syslems suggcss]that thc [urovcr  0[ mcmbranc lipids and thc activity of phosphorylating cnzyme syslcm (prolein kinase C) may bc closely linked t0 nicotine reccptor funclion in ihe periphcra) bcing planned systcm: pilot study ncrous collaboralion with pcrsonnel in Ihe Dcpartment of Biochemistry al BGSM, I0 determine whether slmilar link cxists in Ibe brain; 1 8
To: John H Rcynolds Subject: Highlights Dalc: Scplember 2 1986 From: RM Lippicllo Tcsting ol polentia! ncw ligands for nicoline reccplor binding studics conlinucd: N-melhyl cylisice inas yithesizcd by _D5: Toras Hudlicky (VFI) anc forarded t0 RJR for asscssmcn ot Ils potzngy in inhibition binding assay3 This compound was found to be approximately 100-fold less elicctivc in inhibiting (3HJ-nicotine binding (0 rat brain tissue than its parent compound, L-Eolinc in cylisinc, and 1S-told Iess potent than dolng Thcrcforc, the N-mcthyl derivalive docs nOt appcar (8 be suitable a5 potcntia) ndioligard for nicotine reccpto; characterization: Thc synthcsis of halogenated derivatives 0l Gylisine will now be undcrtakcn: 2 Repurification o L[3H] nicotinc, routinely utilized in nicoline receplor studics, because Rias bcamc ncccssary ound that commercially available material containcd 13-18 % radiochcmicl impuritics. Recent cvidence in the literaturc, based model ccll syslems suggcss]that thc [urovcr  0[ mcmbranc lipids and thc activity of phosphorylating cnzyme syslcm (prolein kinase C) may bc closely linked t0 nicotine reccptor funclion in ihe periphcra) ncrous systcm: pilot study bcing planned collaboralion with pcrsonnel in Ihe Dcpartment of Biochemistry al BGSM, I0 determine whether link cxists in Ibe brain; slmilar 1 8