FSL0833
- Structure
- InChI=1S/C33H40N2O9/c1-38-19-7-8-20-21-9-10-35-16-18-13-27(44-32(36)17-11-25(39-2)30(41-4)26(12-17)40-3)31(42-5)28(33(37)43-6)22(18)15-24(35)29(21)34-23(20)14-19/h7-8,11-12,14,18,22,24,27-28,31,34H,9-10,13,15-16H2,1-6H3/t18-,22+,24-,27-,28+,31+/m1/s1
- InChIKey=QEVHRUUCFGRFIF-MDEJGZGSSA-N
- Synonyms
-
- Origin
- Rauvolfia serpentina
- Biological activities
- Inhibition of vesicular uptake of neurotransmitters, catecholamine and serotonin
- Therapeutic
-
Antihypertensive
Antipsychotic
- Target
-
Vesicular monoamine transporter (VMAT)
- Assay information
-
Binding to VMAT with high affinity (Kd = 30 pM)
Inhibitor of [3H] dopamine uptake in cromaffin granuels (IC50 = 37 nM)
Inhibitor of [3H] norepinephrine transport (IC50 = 9.5 nM) (Kiap = 4.8 μM)
Inhibitor of vesicular monoamine transporter
- References
-
-
Sievert MK, Hajipour AR, Ruoho AE
Specific derivatization of the vesicle monoamine transporter with novel carrier-free radioiodinated reserpine and tetrabenazine photoaffinity labels.
Anal Biochem, 367(1): 68-78 (2007) 17559790 doi: 10.1016/j.ab.2007.04.046
-
Imming P, Sinning C, Meyer A
Drugs, their targets and the nature and number of drug targets.
Nat Rev Drug Discov, 5(10): 821-834 (2006) 17016423 doi: 10.1038/nrd2132
-
Naudon L, Leroux-Nicollet I, Raisman-Vozari R, Botton D, Costentin J
Time-course of modifications elicited by reserpine on the density and mRNA synthesis of the vesicular monoamine transporter, and on the density of the membrane dopamine uptake complex.
Synapse, 21(1): 29-36 (1995) 8525459 doi: 10.1002/syn.890210105
-
Schuldiner S, Liu Y, Edwards RH
Reserpine binding to a vesicular amine transporter expressed in Chinese hamster ovary fibroblasts.
J Biol Chem, 268(1): 29-34 (1993) 8416935
-
Deupree JD, Weaver JA
Identification and characterization of the catecholamine transporter in bovine chromaffin granules using [3H]reserpine.
J Biol Chem, 259(17): 10907-10912 (1984) 6469989
-
FURLENMEIER A, LUCAS R, MACPHILLAMY HB, MULLER JM, SCHLITTLER E
On the constitution of reserpine.
Experientia, 9(9): 331-333 (1953) 13107654