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Title:  Agent for expression of long-term potentiation of synaptic transmission comprising compound having brain somatostatin activation property

United States Patent:  6,344,358

Inventors:  Matsuoka; Nobuya (Ikoma, JP); Satoh; Masamichi (Kyoto, JP)

Assignee:  Fujisawa Pharmaceutical Co., Ltd. (Osaka, JP)

Appl. No.:  321745

Filed:  May 28, 1999

Abstract

The present invention relates to an agent for the expression of long-term potentiation of synaptic transmission, which contains a compound having a brain somatostatin activation property as an active ingredient and to a screening method of an agent for the expression of long-term potentiation of synaptic transmission, which uses a soniatostatin releasing property as an index. The present invention is useful for the prophylaxis and/or treatment of cerebral diseases of dementia, amnesia, manic-depressive psychosis, schizophrenia, Parkinson's disease, psychosomatic disease and the like.

SUMMARY OF THE INVENTION

As a result of the intensive studies of the present inventors, it has been newly found that a compound having a brain somatostatin release promotion property expresses long-term potentiation of synaptic transmission. Based on this new finding, we have found that administration of a compound having a brain somatostatin release promoting property leads to the prophylaxis and/or treatment of cerebral diseases such as dementia, amnesia, manic-depressive psychosis, schizophrenia, Parkinson's disease, psychosomatic disease, and the like, which resulted in the completion of the present invention.

Accordingly, the present invention provides the following.

(1) An agent for expression of long-term potentiation of synaptic transmission, which comprises a compound having a brain somatostatin activation property as an active ingredient.

(2) The agent for expression of long-term potentiation of synaptic transmission of (1), wherein the compound exerts an action to promote a release of brain somatostatin through suppression of a negative feedback mechanism of brain somatostatin release.

(3) The agent for expression of long-term potentiation of synaptic transmission of (1) or (2), which is an agent for the prophylaxis or treatment of cerebral diseases.

(4) The agent for expression of long-term potentiation of synaptic transmission of (3), which is an agent for the prophylaxis or treatment of dementia or amnesia.

(5) A method for expressing long-term potentiation of synaptic transmission, comprising administering an effective amount of a compound having a brain somatostatin activating property.

(6) The method for expressing long-term potentiation of synaptic transmission of (5), wherein the compound exerts an action to promote a release of brain somatostatin through suppression of a negative feedback mechanism of brain somatostatin release.

(7) The method for expressing long-term potentiation of synaptic transmission of (5) or (6), which is a method for the prophylaxis or treatment of cerebral diseases.

(8) The method for expressing long-term potentiation of synaptic transmission of (5) or (6), which is a method for the prophylaxis and/or treatment of dementia or amnesia

(9) Use of a compound having a brain somatostatin activation property for the production of an agent for the expression of long-term potentiation of synaptic transmission.

(10) The use of a compound having a brain somatostatin activation property according to (9), wherein the compound exerts an action to promote a release of brain somatostatin through suppression of a negative feedback mechanism of brain somatostatin release.

(11) The use of a compound having a brain somatostatin activation property according to (9) or (10), which is for the production of an agent for the prophylaxis and/or treatment of cerebral diseases.

(12) The use of a compound having a brain somatostatin activation property according to (9) or (10), which is for the production of an agent for the prophylaxis and/or treatment of dementia or amnesia.

(13) A method for screening an agent for expression of long-term potentiation of synaptic transmission, which comprises using a somatostatin releasing action as an index

(14) The screening method of (13), which is a screening method of an anti-dementia agent or anti-amnesia agent.

(15) A method for screening an agent for expression of long-term potentiation of synaptic transmission, which comprises stimulating hippocampal slices, bringing a hippocampal slice into contact with a test compound, measuring an amount of somatostatin released from the hippocampal slice and/or a release time thereof, measuring an amount of somatostatin released from a hippocampal slice and/or a release time thereof in the absence of a contact with the test compound, and comparing the amounts and/or the times to calculate the amount of somatostatin released from the hippocampal slice and/or the release time thereof caused by the contact with the test compound.

(16) The screening method according to (15), which is a screening method of an anti-dementia agent or anti-amnesia agent.

(17) The agent for expression of long-term potentiation of synaptic transmission of (1), wherein the compound having the brain somatostatin activation property is a compound obtained by the screening method of any of (13) to (16).

(18) The method for expressing long-term potentiation of synaptic transmission according to (5), wherein the compound having the brain somatostatin activation property is a compound obtained by the screening method of any of (13) to (16).

(19) The use of a compound having a brain somatostatin activation property according to (9), wherein the compound having the brain somatostatin activation property is obtained by the screening method of any of (13) to (16).

(20) A compound selected by the screening method described in any of (13) to (16).

Claim 1 of 10 Claims

What is claimed is:

1. A method for expressing long-term potentiation of synaptic transmission, comprising:

administering to a tissue in need thereof, an effective amount of a compound exerting an action to promote release of a brain somatostatin through suppression of a negative feedback mechanism of brain somatostatin release,

with the proviso that the compound is not a compound of formula (I): 

                    

wherein R1 is lower alkyl, aryl, ar(lower)alkoxy or a heterocyclic group, each of which may be substituted with halogen,

R2 is a hydrogen atom or lower alkyl,

R3 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen,

A is --CO--, --SO2 -- or lower alkylene, and

Y is --CO--, --SO2 -- or --CONH--.

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If you want to learn more about this patent, please go directly to the U.S. Patent and Trademark Office Web site to access the full patent.

 

 

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