NNC 45-0095

    Add links
    From Wikipedia, the free encyclopedia
    NNC 45-0095
    NNC 45-0095.svg
    Clinical data
    Other namesNNC-450095
    Drug classSelective estrogen receptor modulator
    Identifiers
    • 4-(1-ethylpyrrolo[2,1,5-cd]indolizin-2-yl)phenol
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC18H15NO
    Molar mass261.324 g·mol−1
    3D model (JSmol)
    • CCC1=C(C2=CC=C3N2C1=CC=C3)C4=CC=C(C=C4)O
    • InChI=1S/C18H15NO/c1-2-15-16-5-3-4-13-8-11-17(19(13)16)18(15)12-6-9-14(20)10-7-12/h3-11,20H,2H2,1H3
    • Key:GBHFDPQPLXKNIU-UHFFFAOYSA-N

    NC 45-0095 is a synthetic nonsteroidal selective estrogen receptor modulator (SERM) which was under development by Novo Nordisk for the treatment of postmenopausal osteoporosis but was never marketed.[1][2][3][4][5] It is a partial agonist of the estrogen receptor (IC50 (for binding inhibition) = 9.5 nM; EC50 = 13 nM) with mixed estrogenic and antiestrogenic activity, and shows full estrogenic activity in bone and uterus (Emax (relative to moxestrol, in Ishikawa endometrial cancer cell line) = 105%).[1][4] The compound is a pyrroloindolizine derivative.[1][2] Its development was discontinued by 2003.[5]

    See also[edit]

    References[edit]

    1. ^ a b c Jørgensen AS, Jacobsen P, Christiansen LB, Bury PS, Kanstrup A, Thorpe SM, Bain S, Naerum L, Wassermann K (February 2000). "Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor". Bioorg. Med. Chem. Lett. 10 (4): 399–402. doi:10.1016/S0960-894X(00)00015-9. PMID 10714509.
    2. ^ a b Sharma, Vikas; Kumar, Vipin (2014). "Indolizine: a biologically active moiety". Medicinal Chemistry Research. 23 (8): 3593–3606. doi:10.1007/s00044-014-0940-1. ISSN 1054-2523. S2CID 2643469.
    3. ^ Wallace OB, Richardson TI, Dodge JA (2003). "Estrogen receptor modulators: relationships of ligand structure, receptor affinity and functional activity". Curr Top Med Chem. 3 (14): 1663–82. doi:10.2174/1568026033451727. PMID 14683521.
    4. ^ a b Atta-ur- Rahman; Allen B. Reitz (10 December 2010). Frontiers in Medicinal Chemistry. Bentham Science Publishers. pp. 206–. ISBN 978-1-60805-205-9.
    5. ^ a b "NNC 450095 - AdisInsight".

    External links[edit]



    Stub icon

    This drug article relating to the genito-urinary system is a stub. You can help Wikipedia by expanding it.

    Retrieved from "https://en.wikipedia.org/w/index.php?title=NNC_45-0095&oldid=1135138833"