US2012196301A1PendingUtilityA1
Use of binding partners for 5-ht5 receptors for the treatment of neurodegenerative and neuropsychiatric disorders
Assignee: GARCIA-LADONA FRANCISCO JAVIERPriority: Jan 11, 1999Filed: Nov 15, 2011Published: Aug 2, 2012
Est. expiryJan 11, 2019(expired)· nominal 20-yr term from priority
A61P 9/10A61P 35/00A61P 25/08A61P 25/00G01N 33/566A61K 31/519A61P 25/18G01N 2500/02A61P 25/28G01N 2500/04
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Claims
Abstract
The present invention relates to the use of binding partners for 5-HT5 receptors for the treatment of neuropathological, in particular neurodegenerative and/or neuropsychiatric, disorders, which can occur, in particular, in cerebral ischemia, stroke, epilepsy and seizures in general, chronic schizophrenia, other psychotic disorders, dementia, in particular Alzheimer's dementia, demyelinizing disorders, in particular multiple sclerosis, and brain tumors. The invention also relates to processes for the identification and characterization of such binding partners, in particular in the form of screening processes.
Claims
exact text as granted — not AI-modified1 . The use of at least one binding partner for 5-HT5 receptors for the preparation of an agent for the treatment of neuropathological disorders and associated indications, symptoms and dysfunctions.
2 . The use as claimed in claim 1 in cerebral ischemia, stroke, epilepsy and attacks in general, chronic schizophrenia, other psychotic disorders, dementia, in particular Alzheimer's dementia, demyelinizing disorders, in particular multiple sclerosis, and brain tumors.
3 . The use as claimed in claim 1 or 2 , wherein the K i values of the binding partner for its binding to 5-HT5 receptors are less than 10- 6 M, preferably less than 10- 7 M and in particular less than 10- 8 M.
4 . The use as claimed in one of claims 1 to 3 , wherein the binding affinity of the binding partner for 5-HT5 receptors is greater than for one or more 5-HT receptors other than 5-HT5.
5 . The use as claimed in one of the preceding claims, wherein the binding affinity of the binding partner for 5-HT5 receptors is greater than for 5-HT1A, 5-HT1D and/or 5-HT1B receptors.
6 . The use as claimed in one of the preceding claims, wherein the binding partner competitively inhibits the binding of 5-CT to 5-HT5 receptors.
7 . A process for the determination of the affinity of binding partners for 5-HT5 receptors, where the binding partner is brought into contact with cell systems having 5-HT5 receptors and the binding affinity is determined.
8 . A process for the determination of the activity of binding partners for 5-HT5 receptors, where the binding partner is brought into contact with cell systems having 5-HT5 receptors and at least one binding partner-induced action is determined.
9 . A process as claimed in claim 8 , where the binding of GTP to G proteins, intracellular calcium levels, the phospholipase C activity and/or the cAMP production are determined.
10 . A process as claimed in either claim 8 or 9 , wherein human glioma cell lines or h5-HT5-transfected heterologous cell lines are used.
11 . A process as claimed in claim 10 , wherein h5-HT5-transfected CHO cells, h5-HT5-transfected human kidney cells, or h5-HT5-transfected C-6 glioma cells are used.
12 . An in vitro screening process for the identification of a 5-HT5 receptor binding partner, where at least one process as claimed in claims 7 to 11 is used.
13 . A process as claimed in claim 12 for the identification of binding partners as defined in claims 1 to 6 .Cited by (0)
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