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Immunoreactive-beta-endorphin, -adrenocorticotropin and -calcitonin in extracts of anaplastic or differentiated (rat) medullary thyroid carcinoma.
Authors:T Shibasaki  L Deftos  R Guillemin
Institution:Department of Biochemistry, University of Colorado Medical School, Denver, Colorado 80262 USA
Abstract:Fifteen analogs of luliberin (2, LRH) were synthesized by the solid phase method and examined for their ability to block ovulation in the rat. Two analogs, Ac-DAla1,DPhe2,DTrp3,6]-LRH and Ac-DPhe1,DPhe2,DTrp3,6]-LRH, each blocked ovulation at a single injection dose of 250 μg administered at noon on the day of proestrus; three peptides, Ac-DPro1,DPhe2,DTrp3,6]-LRH, Ac-DThi1,DPhe2,DTrp3,6]-LRH and Ac-DTrp1,DPhe2,DTrp3,6]-LRH, were effective at doses of 500 μg each; and four others, Ac-DTrp1,DPhe2,DTrp3,DTrp(Nps)6]-LRH, Chlorambucil-DPhe1, DPhe2, DTrp3,6]-LRH, 1,DThi2,DTrp3,6]-LRH and (2-DLys6]-LRH, gave partial inhibition at doses tested.
Keywords:LRH  Luliberin  gonadotropin releasing hormone  MBHA  Boc  DCC  dicyclohexylcarbodiimide  DCM  dichloromethane  TFA  trifluoroacetic acid  TEA  triethyl amine  DMF  dimethylformamide  Tos  Dns  5-dimethylaminonaphthalenesulfonyl (Dansyl)  Chl  4-N  N-bis(2-chloroethyl)aminophenylbutyryl (Chlorambucil)  Bzl  benzyl  Brz  2-bromobenzyloxycarbonyl  Nps  2-nitrophenylsulfenyl  Trp(Nps)  2-(2-nitrophenylsulfenyl)tryptophan  CCD  countercurrent distribution  TLC  thin layer chromatography  HPLC  high pressure liquid chromatography  Thi  β-(2-thienyl)-alanine  Boc-ON  Ac  acetyl    pyroglutamyl  ACTH  adrenocorticotropic hormone
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