TABLE 3.
CNS expression and transport substrates for OATP/Oatp isoforms
| Human OATP Isoform | CNS Expressiona | Rodent Ortholog | CNS Expressiona | Potential Substrate Drugsb |
|---|---|---|---|---|
| OATP1A2 | BBB (ap, bl), possibly glial (detected in glioma) | Oatp1a1 | Choroid plexus (ap) | HMG CoA reductase inhibitors (e.g., atorvastatin, cerivastatin, fluvastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin acid); opioid analgesic peptides (e.g., DPDPE) |
| Oatp1a4 | BBB (ap, bl), choroid plexus | |||
| Oatp1a5 | Choroid plexus (ap), neurons | |||
| Oatp1a6 | Choroid plexus | |||
| OATP1C1 | Detected in brain but localization not confirmed; possibly glial (detected in glioma) | Oatp1c1 | BBB (ap) | Substrate profile restricted to thyroid hormones and conjugated sterols |
| OATP2A1 | Detected in brain but localization not confirmed | Oatp2a1 | BBB (ap), neurons | Substrate profile restricted to prostaglandins |
| OATP2B1 | Detected in brain but localization not confirmed; possibly glial (detected in glioma) | Oatp2b1 | Neurons | HMG CoA reductase inhibitors (e.g., atorvastatin, fluvastatin, pravastatin, pitavastatin, rosuvastatin) |
| OATP3A1_v1, OATP3A2_v2 | Choroid plexus (bl), choroid plexus (ap), neurons (cell body and axon) | Oatp3a1 | Astrocytes | Endogenous opioids (e.g., deltorphin II) |
| OATP4A1 | Detected in brain but localization not confirmed; possibly glial (detected in glioma) | Oatp4a1 | Choroid plexus | Substrate profile restricted to benzylpenicillin, thyroid hormones, prostaglandins, and estrogen metabolites |
| OATP6A1 | Detected in brain but localization not confirmed | Rodent orthologs not detected in CNS tissue | N.A. | Transport activity not yet assessed |
N.A., not applicable.
a
Specific localization, if known, is demarcated as apical (ap) or basolateral (bl).
b
Drugs listed are only those with known efficacy in treatment of pain or cerebral hypoxia.