Events6th International Electronic Conference on Medicinal Chemistry
Event submissions
Published
with-doi10.3390/ECMC2020-07483
This submission belongs to the session B. General: Posters of the event 6th International Electronic Conference on Medicinal Chemistry
Published date
06 Nov, 2020
Citation
Ana Lago-Fernandez, Nadine Jagerovic, Paula Morales, Patricia H. Reggio, Dow P. Hurst, Mary E. Abood, Eugen Brailou, Pingwei Zhao, Luciana M. Leo, Noori Sotudeh, Exploring the orphan GPCR GPR18 through novel synthetic cannabidiol derivatives, in Proceedings of 6th International Electronic Conference on Medicinal Chemistry, 1 November–30 November 2020, MDPI: Basel, Switzerland, doi: 10.3390/ECMC2020-07483
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Exploring the orphan GPCR GPR18 through novel synthetic cannabidiol derivatives

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Ana Lago-Fernandez 1
Pingwei Zhao 2
Noori Sotudeh 3
Luciana M. Leo 2
Eugen Brailou 2
Dow P. Hurst 3
Paula Morales 4
Patricia H. Reggio 3
Mary E. Abood 2
Nadine Jagerovic 4
1. Instituto de Química Médica, Consejo Superior de Investigaciones Científicas, Madrid, Spain, Spain
2. Center for Substance Abuse Research, Temple University, Philadelphia, USA
3. Center for Drug Discovery, University North Carolina Greensboro, USA
4. Instituto de Química Médica, Consejo Superior de Investigaciones Científicas, Madrid, Spain
Abstract

GPR18 is an orphan G-protein coupled receptor (GPCR) mainly expressed in both central and lymphoid tissues that participates in a myriad of physiological functions such as intraocular pressure, cellular migration, apoptosis, nociception or immunomodulation. Hence, this receptor constitutes a very interesting therapeutic target. While numerous cannabinoid ligands have been reported to stimulate GPR18 – including NAGly, Abn-CBD and Δ9-THC – few synthetic compounds have been designed to modulate this GPCR.

Based on an in silico model of GPR18, a series of new compounds with a cannabinoid-like scaffold have been designed and synthesized. Pharmacological evaluation has shown that several of these new compounds were able to activate GPR18 in calcium mobilization studies, whereas others strongly antagonized the effect of NAGly in these assays.

Keywords
GPR18
orphan GPCR
synthetic cannabinoids
Oral Presentation
6_ecmc-5_Poster_template.pptx
Poster
6_ecmc-5_Poster_template.pdf
6_ecmc-5_Poster_template.pdf
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