Abstract
Serotonin is a monoamine serving as a chemical messenger in diverse brain regions, as well as in blood and various other organs. We synthesized six ethylamine functionalized fluorophores as fluorescent probes for serotonin. The one with best spectral properties and aqueous solubility, 6-amino-2-(2- aminoethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione, was studied in detail both in vivo and in vitro. It was shown to act as a ligand for serotonin transporter (SERT) without acute cerebral or cardiovascular toxicity or adverse effects. Fluorescent serotonin analogs can be used for direct visualization of SERT distribution and activity in live tissue.
| Original language | English |
|---|---|
| Pages (from-to) | 7387-7391 |
| Number of pages | 5 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 21 |
| Issue number | 24 |
| DOIs | |
| State | Published - Dec 15 2011 |
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Keywords
- Fluorescent analogs
- Monoamine transporter
- Neurotransmitter
- Reuptake inhibitor
- Serotonin
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry
- Molecular Medicine
- Molecular Biology
- Clinical Biochemistry
- Biochemistry
Cite this
Fluorescent reporters of monoamine transporter distribution and function. / Bagale, Sharanappa M.; Brown, Adrienne S.; Carballosa Gonzalez, Melissa M.; Vitores, Alberto; Micotto, Teresa L.; Saleesh Kumar, N. S.; Hentall, Ian; Wilson, James N.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 24, 15.12.2011, p. 7387-7391.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Fluorescent reporters of monoamine transporter distribution and function
AU - Bagale, Sharanappa M.
AU - Brown, Adrienne S.
AU - Carballosa Gonzalez, Melissa M.
AU - Vitores, Alberto
AU - Micotto, Teresa L.
AU - Saleesh Kumar, N. S.
AU - Hentall, Ian
AU - Wilson, James N
PY - 2011/12/15
Y1 - 2011/12/15
N2 - Serotonin is a monoamine serving as a chemical messenger in diverse brain regions, as well as in blood and various other organs. We synthesized six ethylamine functionalized fluorophores as fluorescent probes for serotonin. The one with best spectral properties and aqueous solubility, 6-amino-2-(2- aminoethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione, was studied in detail both in vivo and in vitro. It was shown to act as a ligand for serotonin transporter (SERT) without acute cerebral or cardiovascular toxicity or adverse effects. Fluorescent serotonin analogs can be used for direct visualization of SERT distribution and activity in live tissue.
AB - Serotonin is a monoamine serving as a chemical messenger in diverse brain regions, as well as in blood and various other organs. We synthesized six ethylamine functionalized fluorophores as fluorescent probes for serotonin. The one with best spectral properties and aqueous solubility, 6-amino-2-(2- aminoethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione, was studied in detail both in vivo and in vitro. It was shown to act as a ligand for serotonin transporter (SERT) without acute cerebral or cardiovascular toxicity or adverse effects. Fluorescent serotonin analogs can be used for direct visualization of SERT distribution and activity in live tissue.
KW - Fluorescent analogs
KW - Monoamine transporter
KW - Neurotransmitter
KW - Reuptake inhibitor
KW - Serotonin
UR - http://www.scopus.com/inward/record.url?scp=81255153664&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=81255153664&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2011.10.007
DO - 10.1016/j.bmcl.2011.10.007
M3 - Article
C2 - 22047697
AN - SCOPUS:81255153664
VL - 21
SP - 7387
EP - 7391
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 24
ER -