Psychoactive substances belonging to the amphetamine class potently activate brain carbonic anhydrase isoforms VA, VB, VII, and XII

Andrea AngeliDipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Florence, Italy;

Fabio VaianoForensic Toxicology Division, Department of Health Sciences, University of Florence, Florence, Italy

Francesco MariForensic Toxicology Division, Department of Health Sciences, University of Florence, Florence, Italy

Elisabetta BertolForensic Toxicology Division, Department of Health Sciences, University of Florence, Florence, ItalyCorrespondenceelisabetta.bertol@unifi-it

Claudiu T. SupuranDipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Florence, Italy; Correspondence[email protected]

Figures & data

Figure 1. Examples of CAAs: histamine 1, histidine 2, phenylalanine 3, (both L- and D-enantiomers possess this activity), and L-adrenaline 4.

Figure 2. Binding of histamine 1 (magenta, PDB ID: 1AVN)Citation⁵ and L-adrenaline (yellow, PDB ID: 2HKK)Citation²⁰ 4 to hCA II, as determined by X-ray crystallography. The Zn(II) ion from the enzyme active site is the magenta sphere, with its three His ligands in green (His94, 96, and 119). His64, the natural proton shuttling residues, is shown (in green) in both its “in” and “out” conformations, above the activator molecules, which are bound at the entrance of the cavity.

Figure 2. Binding of histamine 1 (magenta, PDB ID: 1AVN)Citation5 and L-adrenaline (yellow, PDB ID: 2HKK)Citation20 4 to hCA II, as determined by X-ray crystallography. The Zn(II) ion from the enzyme active site is the magenta sphere, with its three His ligands in green (His94, 96, and 119). His64, the natural proton shuttling residues, is shown (in green) in both its “in” and “out” conformations, above the activator molecules, which are bound at the entrance of the cavity.

Figure 3. Structure of psychoactive substances investigated as CAAs in the present article: amphetamine 5, methamphetamine 6, phentermine 7, mephentermine 8, and chlorphenteramine 9.

Table 1. CA activation of isoforms hCA I, II, VII, and XIII (cytosolic) and IV (membrane-associated) with compounds 1–9, by a stopped-flow CO₂ hydrase assayCitation²⁸.

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Table 2. CA activation of isoforms hCA VA, VB (mitochondrial), VI (secreted), and IX, XII, and XIV (trans-membrane) with compounds 1–9, by a stopped-flow CO₂ hydrase assayCitation²⁸.

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Psychoactive substances belonging to the amphetamine class potently activate brain carbonic anhydrase isoforms VA, VB, VII, and XII

Table 1. CA activation of isoforms hCA I, II, VII, and XIII (cytosolic) and IV (membrane-associated) with compounds 1–9, by a stopped-flow CO₂ hydrase assayCitation²⁸.

Table 2. CA activation of isoforms hCA VA, VB (mitochondrial), VI (secreted), and IX, XII, and XIV (trans-membrane) with compounds 1–9, by a stopped-flow CO₂ hydrase assayCitation²⁸.

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Psychoactive substances belonging to the amphetamine class potently activate brain carbonic anhydrase isoforms VA, VB, VII, and XII

Figures & data

Table 1. CA activation of isoforms hCA I, II, VII, and XIII (cytosolic) and IV (membrane-associated) with compounds 1–9, by a stopped-flow CO2 hydrase assayCitation28.

Table 2. CA activation of isoforms hCA VA, VB (mitochondrial), VI (secreted), and IX, XII, and XIV (trans-membrane) with compounds 1–9, by a stopped-flow CO2 hydrase assayCitation28.

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Table 1. CA activation of isoforms hCA I, II, VII, and XIII (cytosolic) and IV (membrane-associated) with compounds 1–9, by a stopped-flow CO₂ hydrase assayCitation²⁸.

Table 2. CA activation of isoforms hCA VA, VB (mitochondrial), VI (secreted), and IX, XII, and XIV (trans-membrane) with compounds 1–9, by a stopped-flow CO₂ hydrase assayCitation²⁸.