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  • 1
    Electronic Resource
    Electronic Resource
    The structural features of effective antagonists of the luteinizing hormone releasing hormone (1994)
    Springer
    Amino acids 6 (1994), S. 111-130 
    Details
    ISSN: 1438-2199
    Keywords: Amino acids ; LHRH antagonists ; Histamine release ; Structure-activity relationship
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The structure-activity data of 6 years on 395 analogs of the luteinizing hormone releasing hormone (LHRH) have been studied to determine effective substituents for the ten positions for maximal antiovulatory activity and minimal histamine release. The numbers of substituents studied in the ten positions are as follows: (41)1-(12)2-(12)3-(5)4-(47)5-(52)6-(16)7-(18)8-(4)9-(8)10. In position 1, DNal and DQal were effective with the former being more frequently the better substituent. DpClPhe was uniquely effective in position 2. Positions 3 and 4 are very sensitive to change. D3Pal in position 3 and Ser in position 4 of LHRH were in the best antagonists. PicLys and cPzACAla were the most successful residues in position 5 with cPzACAla being the better substituent. Position 6 was the most flexible and many substituents were effective; particularly DPicLys. Leu7 was most often present in the best antagonists. In position 8, Arg was effective for both antiovulatory activity and histamine release; ILys was effective for potency and lesser histamine release. Pro9 of LHRH was retained. DAlaNH2 10 was in the best antagonists.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00805840
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Effective antagonists of luteinizing hormone releasing hormone modified at position one (1993)
    Springer
    Amino acids 5 (1993), S. 359-365 
    Details
    ISSN: 1438-2199
    Keywords: Amino acids ; LHRH antagonists ; Antiovulatory activity ; Histamine release ; Solid phase peptide synthesis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The amino acid, D-2-naphthylalanine, has been used by many investigators as a substituent for position one of antagonists of LHRH. We have newly designed substituents for position one in which the carboxy groups of 2-naphthoic acid, 3-quinoline- and 2-quinoxaline-carboxylic acids are linked to the five amino acids, DAla, DThr, DNVal, DSer, and Gly. The substituents in positions 2–10 were DpClPhe2, DPal3, Ser4, PicLys5, DPicLys6, Leu7, ILys8, Pro9, DAlaNH2 10. Remarkably, DThr, acylated on the amino group by 3-quinolinecarboxylic acid or by 3-quinoxalinecarboxylic acid, and introduced into position one of a relatively potent antagonist, gave a new class of antagonists of LHRH, which released as little histamine as yet recorded, and yet possessed reasonable antiovulatory activity and greatly improved solubility. These structure-activity results advance the basic knowledge of understanding the structural features of such decapeptides which cause antiovulatory activity and histamine release.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00806954
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
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