Derivatives of N,N-diethyl-N′-phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

Derivatives of N,N-diethyl-N′-phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

Derivatives of N,N-diethyl-N′-phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

The present invention relates to agonists of the 5-HT.sub.2A serotonin receptors and their medical uses. In one aspect the invention relates to 5-HT.sub.2A agonists of formula (I). In second aspect, the invention relates to selective 5-HT.sub.2A agonists of formula (II). In another aspect, the invention relates to mixed 5-HT.sub.2A/5-HT.sub.2C agonists of formula (III). In yet another aspect, the invention relates to 5-HT.sub.2A agonists for use in the treatment of a depressive disorder, more particular a 5-HT.sub.2A agonist for the use in the treatment of treatment-resistant depression.

The present invention relates to agonists of the 5-HT.sub.2A serotonin receptors and their medical uses. In one aspect the invention relates to 5-HT.sub.2A agonists of formula (I). In second aspect, the invention relates to selective 5-HT.sub.2A agonists of formula (II). In another aspect, the invention relates to mixed 5-HT.sub.2A/5-HT.sub.2C agonists of formula (III). In yet another aspect, the invention relates to 5-HT.sub.2A agonists for use in the treatment of a depressive disorder, more particular a 5-HT.sub.2A agonist for the use in the treatment of treatment-resistant depression.

Derivatives of N,N-diethyl-N′-phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

Derivatives of N,N-diethyl-N′-phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

Derivatives of N,N-diethyl-N′-phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are particularly useful for the treatment of itch and other dermal conditions.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are particularly useful for the treatment of itch and other dermal conditions.