USE OF 7-CHLORO-N,N,5-TRIMETHYL-4-OXO-3-PHENYL-3,5-DIHYDRO-4H-PYRIDAZINO[4,5-B] INDOLE-1-ACETAMIDE AS A BIOMARKER OF PERIPHERAL BENZODIAZEPINE RECEPTOR LEVELS
Use of a radiolabelled form of 7-chloro-Λ/,Λ/,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4/-/-pyridazino[4,5-b]indole-1-acetamide as a biomarker for the detection, in an individual, of PBR levels associated with normal and pathological conditions. Method for the detection of PBR levels associated with normal and pathological conditions. Diagnostic kit.
1 . A biomarker for the detection, in an individual, of PBR levels associated with normal and pathological conditions, comprising radiolabelled 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide wherein the radiolabel is chosen among carbon-11, radiohalogens and radiometals.
2 . The biomarker according to claim 1 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with carbon-11.
3 . The biomarker according to claim 1 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with carbon-11 on the carbon of the methyl group located on position 5 of the indole nucleus.
4 . The biomarker according to claim 1 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with radiohalogens.
5 . according to claim 1 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with the radiohalogen fluorine-18.
6 . The biomarker according to claim 5 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with fluorine-18 on the para position of the 3-phenyl ring.
7 . The biomarker according to claim 1 wherein the detection of PBR levels and inflammation is performed by PET imaging (positron emission tomography) or SPECT imaging (single photon emission computed tomography).
8 . The biomarker according to claim 1 wherein the detection of PBR levels and inflammation is performed by PET imaging (positron emission tomography).
9 . The biomarker according to claim 1 wherein pathological conditions related to changes in PBR levels are selected from brain injuries, brain infections and neurological diseases.
10 . The biomarker according to claim 1 wherein pathological conditions related to changes in PBR levels are selected from psychiatric diseases.
11 . The biomarker according to claim 1 wherein pathological conditions related to changes in PBR levels are selected from proliferative diseases.
12 . The biomarker according to claim 1 wherein pathological conditions related to changes in PBR levels are selected from peripheral inflammatory processes.
13 . The biomarker according to claim 1 wherein detection of PBR levels is performed for occupancy studies.
14 . The biomarker according to claim 1 wherein detection of PBR levels is performed for evaluating the efficacy of a therapeutic treatment.
15 . Method for the detection of PBR levels associated with normal conditions and changes in PBR levels associated with pathological conditions wherein the detection is performed using a radiolabelled form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, wherein the radiolabel is chosen among carbon-11, radiohalogens and radiometals.
16 . Method according to claim 15 wherein the radiolabelled form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide contains carbon-11.
17 . Method according to claim 15 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with carbon-11 on the carbon of the methyl group located on position 5 of the indole nucleus.
18 . Method according to claim 15 , wherein 7-chloro-N,N,5-trimethyl-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with fluorine-18.
19 . Method according to claim 15 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with fluorine-18 on the para position of the 3-phenyl ring.
20 . Method according to claim 15 wherein pathological conditions related to changes in PBR levels are selected from brain injuries, brain infections, and neurological diseases.
21 . Method according to claim 15 wherein pathological conditions related to changes in PBR levels are selected from psychiatric diseases.
22 . Method according to claim 15 wherein pathological conditions related to changes in PBR levels are selected from proliferative diseases.
23 . Method according to claim 15 wherein pathological conditions related to changes in PBR levels are selected from peripheral inflammatory processes.
24 . Method according to claim 15 wherein detection of PBR levels is performed for occupancy studies.
25 . Method according to claim 15 wherein detection of PBR levels is performed for evaluating the efficacy of a therapeutic treatment.
26 . Diagnostic kit for the detection of PBR levels associated with normal conditions and changes in PBR levels associated with pathological conditions comprising a radiolabelled form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide.
27 . Method according to claim 15 wherein 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide is radiolabelled with radiohalogens.
28 . Method according to claim 15 wherein the detection of PBR levels and inflammation is performed by PET imaging (positron emission tomography) or SPECT imaging (single photon emission computed tomography).