Florida A&m University

Florida Agricultural and Mechanical University

Seth Y Ablordeppey

Xue You Zhu

Donald M N Sikazwe

Novel dual 5-HT1A and 5-HT7 receptor ligands and methods of using the novel ligands to treat a neurological disorder are presented.

And synthesis of dual 5-HT1A and 5-HT7 receptor ligands

A method of treating psychosis, and the underlying antipsychotic formulation. The method includes administering a therapeutically effective amount of synthetic agents that selectively recruit &#x3b2;-arrestin to D2 receptors and have little-to-no binding to culprit receptors associated with weight gain and Type II diabetes. The synthetic agents can include SYA16263 and SYA16264, and/or derivatives or analogs thereof. The 1-(pyridin-2-yl)piperazine moiety was found to play a significant role in recruiting &#x3b2;-arrestin to D2 receptors. In other embodiments, the current invention relates to synthetic agents that are selective of D4 receptors for treatment of psychosis and erectile dysfunction. The synthetic agents can include SYA27287 and/or derivatives or analogs thereof. In all embodiments, extrapyramidal side effects are eliminated or minimized.

Identification of agents displaying functional activation of dopamine D2 and D4 receptors

Derivatives of 1,2,3,4-tetrahydroisoquinoline (THIQ) having the general formula A-(CH)&#x2014;B are provided, wherein A is THIQ or a substituted derivative thereof and B is an aryl, cycloalkylaryl, or cycloalkyl group, wherein A and B are linked to each other by an alkyl or substituted alkyl chain. The compounds are useful as selective ligands (agonists or antagonists) of central nervous system receptors, and in particular of the seratonin receptors. The compounds or their salts can be formulated into pharmaceutical in need thereof by any route of administration suitable for a desired treatment protocol and especially for the treatment of psychiatric disorders.

Alkylated tetrahydroisoquinolines for binding to central nervous system receptors

An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N&#x2014;R, O, S, S&#x2550;O, CH, or C&#x2550;O, where Ris a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring. In one embodiment the quarternary N-5 atom is &#x2014;CHand the 10 position is N&#x2014;(CH)-Ph.

Antifungal and antiparasitic indoloquinoline derivatives

The present invention relates to quinolinium antiinfective agents in which the qunolinium nucleus is fused to an indole ring or the qunolinium nucleus is linked to a cyclic structure through an opened indole or a benzothiophene or benzofuran ring. The compound is further substituted with various substituent groups. The compounds are represented by formula (I), (II) and (III):  Pharmaceutical compositions and methods of use are also included.

3-substituted quinolinium and 7H-indolo[2,3-c]quinolinium salts as new antiinfectives

An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N&#x2014;R, O, S, S&#x2550;O, CH, or C&#x2550;O, where Ris a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring. In one embodiment the quarternary N-5 atom is &#x2014;CHand the 10 position is N&#x2014;(CH)&#x2014;Ph.

Antifungal and antiparasitic indoloquinoline derivates

Haloperidol analogs that conforms to the structural formulae:  

Growing community of inventors

Tallahassee, FL, United States of America

Seth Y Ablordeppey