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Transport of Thyrotropin Releasing Hormone in Rabbit Buccal Mucosa in Vitro

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Abstract

The transport of thyrotropin releasing hormone (TRH) in rabbit buccal mucosa in vitro has been investigated with respect to (a) rate and type of metabolism of TRH on mucosal and serosal sides of buccal mucosa, (b) mechanism of TRH transport including charge effect on its permeability, and (c) pathway and rate-limiting regions of TRH movement. In addition, the integrity of excised buccal mucosa has been evaluated for purposes of in vitro solute diffusion experiments using tissue ATP level data, transmission electron microscopy, and TRH transport kinetic data. The results indicate that excised rabbit buccal mucosa can be used for TRH diffusion studies for approximately 6 hr. In addition, TRH apparently traverses buccal mucosa by simple diffusion with a steady-state permeability of about 10−7 cm/sec, and this permeability is independent of pH. Moreover, the primary pathway appears to be via the intercellular space in the rate-limiting barrier, i.e., the upper 50 µm of the epithelium. Finally, TRH is degraded predominantly by deamidase activity, which is followed by, to a lesser degree, carboxypeptidase metabolism.

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Author notes

  1. Kim E. Knuth & Brian K. Irons

    Present address: Columbia Research Labs, 1202 Ann Street, Madison, Wisconsin, 53713

Authors and Affiliations

  1. School of Pharmacy, University of Wisconsin-Madison, Madison, Wisconsin, 53706

    Martin E. Dowty, Kim E. Knuth, Brian K. Irons & Joseph R. Robinson

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Dowty, M.E., Knuth, K.E., Irons, B.K. et al. Transport of Thyrotropin Releasing Hormone in Rabbit Buccal Mucosa in Vitro . Pharm Res 9, 1113–1122 (1992). https://doi.org/10.1023/A:1015883217858

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