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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Review Article

Exploring μ-Opioid Receptor Splice Variants as a Specific Molecular Target for New Analgesics

Author(s): Hirokazu Mizoguchi* and Hideaki Fujii

Volume 20, Issue 31, 2020

Page: [2866 - 2877] Pages: 12

DOI: 10.2174/1568026620666200922113430

Price: $65


Since a μ-opioid receptor gene containing multiple exons has been identified, the variety of splice variants for μ-opioid receptors have been reported in various species. Amidino-TAPA and IBNtxA have been discovered as new analgesics with different pharmacological profiles from morphine. These new analgesics show a very potent analgesic effect but do not have dependence liability. Interestingly, these analgesics show the selectivity to the morphine-insensitive μ-opioid receptor splice variants. The splice variants, sensitive to these new analgesics but insensitive to morphine, may be a better molecular target to develop the analgesics without side effects.

Keywords: μ-Opioid receptor, Splice variant, Narcotic analgesics, Amidino-TAPA, IBNtxA, Molecular target.

Graphical Abstract
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