Homologues and isomers of noladin ether, a putative novel endocannabinoid: Interaction with rat cannabinoid CB1 receptors

Giovanni Appendino; Alessia Ligresti; Alberto Minassi; Nives Daddario; Tiziana Bisogno; Vincenzo Di Marzo

doi:10.1016/S0960-894X(02)00839-9

Homologues and isomers of noladin ether, a putative novel endocannabinoid: Interaction with rat cannabinoid CB₁ receptors

Giovanni Appendino
, Alessia Ligresti
, Alberto Minassi
, Nives Daddario
, Tiziana Bisogno
, Vincenzo Di Marzo

Dipartimento di Scienze del Farmaco

Risultato della ricerca: Contributo su rivista › Articolo in rivista › peer review

Abstract

Two regioisomers and 13 analogues of the putative endocannabinoid noladin ether (2-arachidonyl glyceryl ether, 2-AGE, 1) were synthesized and tested for their interaction with CB₁ receptors in rat brain membranes. The results showed that a C-20 tetra-unsaturated moiety is necessary for high affinity, and that a series of alkyl glyceryl ethers of potential occurrence in brain tissues have less affinity than 2-AGE for CB₁ receptors.

Lingua originale	Inglese
pagine (da-a)	43-46
Numero di pagine	4
Rivista	Bioorganic and Medicinal Chemistry Letters
Volume	13
Numero di pubblicazione	1
DOI	https://doi.org/10.1016/S0960-894X(02)00839-9
Stato di pubblicazione	Pubblicato - 6 gen 2003

Accesso al documento

10.1016/S0960-894X(02)00839-9

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title = "Homologues and isomers of noladin ether, a putative novel endocannabinoid: Interaction with rat cannabinoid CB1 receptors",

abstract = "Two regioisomers and 13 analogues of the putative endocannabinoid noladin ether (2-arachidonyl glyceryl ether, 2-AGE, 1) were synthesized and tested for their interaction with CB1 receptors in rat brain membranes. The results showed that a C-20 tetra-unsaturated moiety is necessary for high affinity, and that a series of alkyl glyceryl ethers of potential occurrence in brain tissues have less affinity than 2-AGE for CB1 receptors.",

author = "Giovanni Appendino and Alessia Ligresti and Alberto Minassi and Nives Daddario and Tiziana Bisogno and \{Di Marzo\}, Vincenzo",

note = "Funding Information: We are grateful to Chemi (Cinisello Balsamo, MI, Italy) for a generous gift of d - and l -solketal, and to Giuseppe Guilla for his help in the synthesis of several glyceryl ethers. Support from MURST (grant 3933 to V.D.M.) is acknowledged.",

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AU - Appendino, Giovanni

AU - Ligresti, Alessia

AU - Minassi, Alberto

AU - Daddario, Nives

AU - Bisogno, Tiziana

AU - Di Marzo, Vincenzo

N1 - Funding Information: We are grateful to Chemi (Cinisello Balsamo, MI, Italy) for a generous gift of d - and l -solketal, and to Giuseppe Guilla for his help in the synthesis of several glyceryl ethers. Support from MURST (grant 3933 to V.D.M.) is acknowledged.

PY - 2003/1/6

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N2 - Two regioisomers and 13 analogues of the putative endocannabinoid noladin ether (2-arachidonyl glyceryl ether, 2-AGE, 1) were synthesized and tested for their interaction with CB1 receptors in rat brain membranes. The results showed that a C-20 tetra-unsaturated moiety is necessary for high affinity, and that a series of alkyl glyceryl ethers of potential occurrence in brain tissues have less affinity than 2-AGE for CB1 receptors.

AB - Two regioisomers and 13 analogues of the putative endocannabinoid noladin ether (2-arachidonyl glyceryl ether, 2-AGE, 1) were synthesized and tested for their interaction with CB1 receptors in rat brain membranes. The results showed that a C-20 tetra-unsaturated moiety is necessary for high affinity, and that a series of alkyl glyceryl ethers of potential occurrence in brain tissues have less affinity than 2-AGE for CB1 receptors.

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