University of North Texas

The United States of America, as Represented by the Secretary, Department of Health and Human Services

Peter Grundt

Amy Hauck Newman

Robert R Luedtke

Jianjing Cao

Jonathan L Katz

George C Cyriac

Robert Leudtke

Dopamine Dreceptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved Dreceptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH or OAc groups have been introduced into the linking chain. In general, these modifications are well tolerated at Dreceptors and achieve high selectivity over Dand Dreceptors.

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A family of structurally rigid dopamine D3 receptor selective ligands is described. The family of structurally rigid dopamine D3 receptor selective ligands has the formula wherein A is cis or trans &#x2014;CH&#x2550;CH&#x2014;, &#x2014;C&#x2550;C&#x2014;, or cyclohexyl. B is cis or trans &#x2014;CH&#x2550;CH&#x2014; or absent. R1 represents an optionally substituted phenyl group, wherein said substituents are selected from the group consisting of: hydrogen, halogen, amino, nitro, hydroxyl, alkoxy, alkyl, acyl and pyridyl, and said substitution may occur at any of the ortho, meta, or para positions, or R1 represents a heteroaromatic ring. A preferred heteroaromatic ring is indole, quinoxoline, pyridyl, pyrimidyl, or imidazole. R2 and R3 may be independently hydrogen or a halogen, or R2 alone may be C1, C2, or C3 alkoxy, and m is 1 or 2, and n is 0, 1, or 2. 

Structurally rigid dopamine D3 receptor selective ligands and process for making them

A family of structurally rigid dopamine D3 receptor selective ligands is described. The family of structurally rigid dopamine D3 receptor selective ligands has the formula wherein A is cis or trans &#x2014;CH&#x2550;CH&#x2014;, &#x2014;C&#x2550;C&#x2014;, or cyclohexyl. B is cis or trans &#x2014;CH&#x2550;CH&#x2014; or absent. R1 represents an optionally substituted phenyl group, wherein said substituents are selected from the group consisting of: hydrogen, halogen, amino, nitro, hydroxyl, alkoxy, alkyl, acyl and pyridyl, and said substitution may occur at any of the ortho, meta, or para positions, or R1 represents a heteroaromatic ring. A preferred heteroaromatic ring is indole, quinoxoline, pyridyl, pyrimidyl, or imidazole. R2 and R3 may be independently hydrogen or a halogen, or R2 alone may be C1, C2, or C3 alkoxy, and m is 1 or 2, and n is 0, 1, or 2.

Structurally rigid dopamine d3 receptor selective ligands and process for making them

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Peter Grundt