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Medical imaging
RTI-51
Другие языки:

    RTI-51

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    RTI-51
    RTI-51.png
    Identifiers
    • methyl (1R,2S,3S,5S)-3-(4-bromophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
    CAS Number
    PubChem CID
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C16H20BrNO2
    Molar mass 338.245 g·mol−1
    3D model (JSmol)
    • Brc1ccc(cc1)[C@H]2C[C@@H]3N(C)[C@H]([C@H]2C(=O)OC)CC3
    • InChI=1S/C16H20BrNO2/c1-18-12-7-8-14(18)15(16(19)20-2)13(9-12)10-3-5-11(17)6-4-10/h3-6,12-15H,7-9H2,1-2H3/t12-,13-,14+,15+/m1/s1 ☒N
    • Key:HNVGNUVAMRLMSG-KBXIAJHMSA-N ☒N
     ☒NcheckY (what is this?)  (verify)

    (–)-2β-Carbomethoxy-3β-(4-bromophenyl)tropane (RTI-4229-51, bromopane) is a semi-synthetic alkaloid in the phenyltropane group of psychostimulant compounds. First publicized in the 1990s, it has not been used enough to have gained a fully established profile. RTI-51 can be expected to have properties lying somewhere in between RTI-31 and RTI-55. Importantly it has a ratio of monoamine reuptake inhibition of D > S > N (1.8:10.6:37.4nM respectively) which is an unusual balance of effects not produced by other commonly used compounds (although RTI-121 is similar, but more DAT selective). It has been used in its 76Br radiolabelled form to map the distribution of dopamine transporters in the brain.

    Comparison of halogens
    Halogen Atomic № Atomic Weight EN Bond Length
    Fluorine 9 19.0 4.0
    Chlorine 17 35.5 3.2
    Bromine 35 79.9 3.0
    Iodine 53 127 2.7

    Modern research seems to confirm the above hypothesis. However, earlier work produced more scattered results. Based upon what is obvious from the table, RTI-31, RTI-51, and RTI-55 are all similarly potent TRIs.

    MAT IC50 (and Ki) for simple phenyltropanes with 1R,2S,3S stereochemistry.
    Compound [3H]CFT [3H]DA [3H]Nisoxetine [3H]NE [3H]Paroxetine [3H]5-HT
    Cocaine 89.1 275 cf. 241 3300 (1990) 119 cf. 161 1050 (45) 177 cf. 112
    WIN 35,065-2 23 49.8 920 (550) 37.2 1960 (178) 173
    WIN 35,428 13.9 23.0 835 (503) 38.6 692 (63) 101
    RTI-31 1.1 3.68 37 (22) 5.86 44.5 (4.0) 5.00
    RTI-113 1.98 5.25 2,926 242 2,340 391
    RTI-51 1.7 ? 37.4 (23) ? 10.6 (0.96) ?
    RTI-55 1.3 1.96 36 (22) 7.51 4.21 (0.38) 1.74
    RTI-32 1.7 7.02 60 (36) 8.42 240 (23) 19.4

    Data in Above table from rats brains (1995). More recent work has advocated using cloned human transporter/s.

    See also


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