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Ex Vivo Feedback Control of Neurotransmission Using a Photocaged Adenosine A1 Receptor Agonist.
Craey, Erine; Hulpia, Fabian; Spanoghe, Jeroen; Manzella, Simona; Larsen, Lars E; Sprengers, Mathieu; De Bundel, Dimitri; Smolders, Ilse; Carrette, Evelien; Delbeke, Jean; Vonck, Kristl; Boon, Paul; Van Calenbergh, Serge; Wadman, Wytse J; Raedt, Robrecht.
Affiliation
  • Craey E; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Hulpia F; Laboratory of Medicinal Chemistry, Department of Pharmaceutics, Ghent University, 9000 Ghent, Belgium.
  • Spanoghe J; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Manzella S; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Larsen LE; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Sprengers M; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • De Bundel D; Research Group Experimental Pharmacology, Department of Pharmaceutical Chemistry, Drug Analysis and Drug Information, Center for Neurosciences, Vrije Universiteit Brussel, 1090 Brussels, Belgium.
  • Smolders I; Research Group Experimental Pharmacology, Department of Pharmaceutical Chemistry, Drug Analysis and Drug Information, Center for Neurosciences, Vrije Universiteit Brussel, 1090 Brussels, Belgium.
  • Carrette E; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Delbeke J; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Vonck K; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Boon P; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Van Calenbergh S; Laboratory of Medicinal Chemistry, Department of Pharmaceutics, Ghent University, 9000 Ghent, Belgium.
  • Wadman WJ; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
  • Raedt R; 4Brain, Department of Head and Skin, Ghent University, 9000 Ghent, Belgium.
Int J Mol Sci ; 23(16)2022 Aug 10.
Article in En | MEDLINE | ID: mdl-36012151
ABSTRACT
We report the design, synthesis, and validation of the novel compound photocaged N6-cyclopentyladenosine (cCPA) to achieve precisely localized and timed release of the parent adenosine A1 receptor agonist CPA using 405 nm light. Gi protein-coupled A1 receptors (A1Rs) modulate neurotransmission via pre- and post-synaptic routes. The dynamics of the CPA-mediated effect on neurotransmission, characterized by fast activation and slow recovery, make it possible to implement a closed-loop control paradigm. The strength of neurotransmission is monitored as the amplitude of stimulus-evoked local field potentials. It is used for feedback control of light to release CPA. This system makes it possible to regulate neurotransmission to a pre-defined level in acute hippocampal brain slices incubated with 3 µM cCPA. This novel approach of closed-loop photopharmacology holds therapeutic potential for fine-tuned control of neurotransmission in diseases associated with neuronal hyperexcitability.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptor, Adenosine A1 / Adenosine A1 Receptor Agonists Language: En Journal: Int J Mol Sci Year: 2022 Document type: Article Affiliation country:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptor, Adenosine A1 / Adenosine A1 Receptor Agonists Language: En Journal: Int J Mol Sci Year: 2022 Document type: Article Affiliation country: