IP Library Granted Patent US 8,647,827
Granted Patent B2
US 8,647,827 · App. 13/111,713 · Granted Feb 11, 2014

Fluorescent substrates for neurotransmitter transporters

Inventors: Randy D. Blakely (Brentwood, TN); John N. Mason (Nashville, TN); Ian D. Tomlinson (Nashville, TN); Sandra J. Rosenthal (Nashville, TN)
Assignee: Vanderbilt University
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Quick Facts
Patent No.
US 8,647,827
App. No.
13/111,713
Granted
Feb 11, 2014
Kind
B2
Abstract

The invention is based on the finding that IDT307 and analogs thereof are fluorescent substrates transported by several neurotransmitter transporters. Provided are methods for the analysis of neurotransmitter transport and binding using IDT307 and its analogs. The invention also provides rapid methods for screening for modulators of neurotransmitter transport.

Claims (14)

1. A kit comprising:

(a) a compound having the formula:

wherein the phenyl ring is unsubstituted or carries one, two, three or four substituents selected independently from C 1-12 alkyl, fluorinated alkyls, nitro, CN, SCN, OCN, amino, N-alkyl amino, N,N-dialkyl amino, F, Br, I, Cl, furyl, thiophenyl, pyridyl, piperidyl, phenyl, napthyl, OH, OR, SH, SR, CONH 2 , CONHR, SO 2 NH 2 , SO 2 NHR, COR, wherein R is C 1-12 alkyl;

wherein the pyridyl ring is unsubstituted or carries one, two three or four substituents selected independently from C 1-12 alkyl, fluorinated alkyls, nitro, CN, SCN, OCN, amino, N-alkyl amino, N,N-dialkyl amino, F, Br, I, Cl, furyl, thiophenyl, pyridyl, piperidyl, phenyl, napthyl, OH, OR, SH, SR, CONH 2 , CONHR, SO 2 NH 2 , SO 2 NHR, COR, wherein R is C 1-12 alkyl;

Z may be alkyl, aryl, or benzyl, in a container; and

(b) one or more monoamine transporter agonists or antagonists in one or more suitable containers.

2. The kit of claim 1 , wherein the monoamine transporter agonist or antagonist is an epinephrine transporter agonist or antagonist.

3. The kit of claim 1 , wherein the monoamine transporter agonist or antagonist is a dopamine transporter agonist or antagonist.

4. The kit of claim 1 , wherein the monoamine transporter agonist or antagonist is a serotonin transporter agonist or antagonist.

5. The kit of claim 1 , wherein both the phenyl ring and the pyridyl ring are unsubstituted, and Z is nPr.

6. The kit of claim 1 , wherein both the phenyl ring and the pyridyl ring are unsubstituted, and Z is ethyl.

7. The kit of claim 1 , wherein both the phenyl ring and the pyridyl ring are unsubstituted, and Z is methyl.

8. The kit of claim 1 , wherein the pyridyl ring is unsubstituted, the phenyl ring comprises a fluorine substituent and Z is methyl.

9. The kit of claim 1 , wherein the pyridyl ring is unsubstituted, the phenyl ring comprises a methyl substituent and Z is methyl.

Assignments (2)
CONFIRMATORY LICENSE Recorded Dec 1, 2016
From: VANDERBILT UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 040483/0250 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 17, 2013
From: BLAKELY, RANDY D.; MASON, JOHN N.; TOMLINSON, IAN D.; ROSENTHAL, SANDRA J.
To: VANDERBILT UNIVERSITY
Reel/Frame 031428/0570 →
Continuity (3)
Division 11832905 · Aug 2, 2007
Provisional Application 60836635 · Aug 9, 2006
Related Publication 20110229910A1 · Sep 22, 2011