Measurement of neural activity
OwnerErik Arstadinventor
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Abstract
The present invention provides a method for determination of neural activity in a sample. The method of the invention is useful for the determination of neural activity in both in vivo and in vitro samples and is particularly useful in providing diagnostic information in subjects suspected to have a neurological condition that leads to disturbed neurological signalling. Also provided by the invention are compounds suitable for use in the method of the invention, and a pharmaceutical composition useful for carrying out the method of the invention.
Claims13
1-24. (canceled)
A method of determining neural activity in an in vivo sample comprising detecting signals emitted by a labelled compound present in said sample, characterised in that said detecting is carried out by SPECT or PET, and wherein said labelled compound has selective affinity for the inactivated or active state of voltage-gated sodium channels.
A labelled compound of Formula I:
- labelled with a detectable label suitable for detecting by SPECT or PET;
- and wherein:
- R1a to R1c are independently an R1 group selected from hydrogen, C1-3 alkyl, C1-3 alkoxy, hydroxyl, C1-3 hydroxyalkyl, thiol, C1-3 thioalkyl, C1-3 thioalkoxy, halo, C1-3 haloalkyl, C1-3 haloalkoxy, nitro, C1-3 nitroalkyl, C1-3 nitroalkoxy, C4-6 cycloalkyl, or a C3-5 heterocycloalkyl group attached via a C1-3 alkyl;
- R2 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, or a C4-6 cycloalkyl group attached via a C1-6 alkyl;
- A is S or O;
- X is C and the dotted bond is a double bond, or X is N and the dotted bond is a single bond;
- and,
- Y is CH2 or CH═CH.
A labelled compound of Formula II:
- labelled with a detectable label suitable for detecting by SPECT or PET and wherein:
- R3 and R4 are independently selected from hydrogen, C1-10 alkyl, C1-10 alkoxy, C1-4 haloalkyl, C1-4 haloalkenyl, C1-3 haloalkoxy;
- C4-6 cycloalkyl, C1-20 PEGalkyl or C1-20 PEG;
- and,
- R5a and R5b are independently an R5 group selected from hydrogen, C1-4 alkyl, halo, C1-3 haloalkenyl, C1-3 alkoxy, or is a 5- or 6-membered aromatic ring system having 0-3 heteroatoms selected from N, S and O and optionally substituted with C1-3 alkyl, halo, or C1-3 haloalkyl.
Dependencies are inferred from the claim text.