5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists

Michel Perez; Petrus Pauwels; Christiane Palmier; Gareth W. John; Jean Pierre Valentin; Serge Halazy

doi:10.1016/0960-894X(95)00091-7

5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT_1D receptor agonists

Michel Perez
, Petrus Pauwels
, Christiane Palmier
, Gareth W. John
, Jean Pierre Valentin
, Serge Halazy

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

New 5-O-carboxymethyl piperazide derivatives of tryptamine (6a-d) have been prepared in 4 steps from serotonin as 5-HT_1D receptors agonists. Binding studies with cloned human 5-HT_1Dα and 5-HT_1Dβ receptors demonstrate that these derivatives are high affinity ligands at both receptor subtypes and inhibition of forskolin mediated cyclase studies with human 5-HT_1Dβ and 5-HT_1A receptors show that these compounds are very efficient and selective 5-HT_1Dβ agonists.

Original language	English
Pages (from-to)	663-666
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	5
Issue number	7
DOIs	https://doi.org/10.1016/0960-894X(95)00091-7
State	Published - 6 Apr 1995
Externally published	Yes

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10.1016/0960-894X(95)00091-7

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title = "5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists",

abstract = "New 5-O-carboxymethyl piperazide derivatives of tryptamine (6a-d) have been prepared in 4 steps from serotonin as 5-HT1D receptors agonists. Binding studies with cloned human 5-HT1Dα and 5-HT1Dβ receptors demonstrate that these derivatives are high affinity ligands at both receptor subtypes and inhibition of forskolin mediated cyclase studies with human 5-HT1Dβ and 5-HT1A receptors show that these compounds are very efficient and selective 5-HT1Dβ agonists.",

author = "Michel Perez and Petrus Pauwels and Christiane Palmier and John, \{Gareth W.\} and Valentin, \{Jean Pierre\} and Serge Halazy",

year = "1995",

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doi = "10.1016/0960-894X(95)00091-7",

language = "English",

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pages = "663--666",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - 5-O-Carboxymethyl piperazide derivatives of serotonin

T2 - a new class of potent and selective 5-HT1D receptor agonists

AU - Perez, Michel

AU - Pauwels, Petrus

AU - Palmier, Christiane

AU - John, Gareth W.

AU - Valentin, Jean Pierre

AU - Halazy, Serge

PY - 1995/4/6

Y1 - 1995/4/6

N2 - New 5-O-carboxymethyl piperazide derivatives of tryptamine (6a-d) have been prepared in 4 steps from serotonin as 5-HT1D receptors agonists. Binding studies with cloned human 5-HT1Dα and 5-HT1Dβ receptors demonstrate that these derivatives are high affinity ligands at both receptor subtypes and inhibition of forskolin mediated cyclase studies with human 5-HT1Dβ and 5-HT1A receptors show that these compounds are very efficient and selective 5-HT1Dβ agonists.

AB - New 5-O-carboxymethyl piperazide derivatives of tryptamine (6a-d) have been prepared in 4 steps from serotonin as 5-HT1D receptors agonists. Binding studies with cloned human 5-HT1Dα and 5-HT1Dβ receptors demonstrate that these derivatives are high affinity ligands at both receptor subtypes and inhibition of forskolin mediated cyclase studies with human 5-HT1Dβ and 5-HT1A receptors show that these compounds are very efficient and selective 5-HT1Dβ agonists.

UR - https://www.scopus.com/pages/publications/0028907260

U2 - 10.1016/0960-894X(95)00091-7

DO - 10.1016/0960-894X(95)00091-7

M3 - Article

AN - SCOPUS:0028907260

SN - 0960-894X

VL - 5

SP - 663

EP - 666

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists

Abstract

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5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT_1D receptor agonists