Effects of dopaminergic compounds on carbonic anhydrase isozymes I, II, and VI

Abstract

Studies on carbonic anhydrase (CA, EC 4.2.1.1) inhibitors have increased due to several therapeutic applications while there are few investigations on activators. Here we investigated CA inhibitory and activatory capacities of a series of dopaminergic compounds on human carbonic anhydrase (hCA) isozymes I, II, and VI. 2-Amino-1,2,3,4-tetrahydronaphthalene-6,7-diol hydrobromide and 2-amino-1,2,3,4-tetrahydronaphthalene-5,6-diol hydrobromide were found to show effective inhibitory action on hCA I and II whereas 2-amino-5,6-dibromoindan hydrobromide and 2-amino-5-bromoindan hydrobromide exhibited only moderate inhibition against both isoforms, being more effective inhibitors of hCA VI. K_i values of the molecules 3–6 were in the range of 41.12–363 μM against hCA I, of 0.381–470 μM against hCA II and of 0.578–1.152 μM against hCA VI, respectively. Compound 7 behaved as a CA activator with K_A values of 27.3 μM against hCA I, of 18.4 μM against hCA II and of 8.73 μM against hCA VI, respectively.

Keywords::

• Carbonic anhydrase
• dopaminergic
• hCA I
• hCA II
• inhibitor

Acknowledgement

This study was financed by Turkish Republic Prime Ministry State Planning Organization (DPT), (project no: 2010K120440) and Ağrı İbrahim Çeçen University Scientific Research Council, (project no: Ağrı BAP-2010/K-10) for (MS), and by an FP7 EU grant (Metoxia), for CTS.

Declaration of interest

The authors report no declarations of interest.