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The search for opiate analogs that retain effective analgesic qualities without detrimental side effects has yielded numerous compounds, including buprenorphine. Early studies of buprenorphine demonstrated analgesic effectiveness with a favorable safety profile, leading to the approval of formulations for use in humans. Since then, advances in receptor theory and molecular cloning of opioid receptors have led to a deeper understanding of buprenorphine pharmacology. More recent studies of receptor affinity and intrinsic activity have shown that buprenorphine is a \u03bc\u2010 and \u03ba\u2010opioid receptor agonist, a nociceptin orphanin peptide agonist, and a \u03b4\u2010opioid receptor antagonist. Buprenorphine appears to have a primary spinal analgesic mechanism with complex supraspinal actions. It is considered a full agonist for pain but a partial agonist for other clinical endpoints such as respiratory depression. In feline medicine, buprenorphine is approved as low\u2010 and high\u2010concentration injectable solutions, in addition to the most recently introduced long\u2010acting transdermal formulation. Several investigational and compounded formulations have also been evaluated. There are contrasting differentiable features that include pharmacokinetics, onsets\u2010 and durations\u2010of\u2010action, routes of administration, and formulation constituents. Available buprenorphine formulations allow clinicians to select a formulation based on the anticipated duration of pain associated with various surgical procedures, and to provide interventions as needed. In light of the newly approved transdermal buprenorphine solution in cats and progress in buprenorphine pharmacology, the objective of this review is to examine the history and pharmacology of buprenorphine relative to full opioid agonists, where appropriate, integrating these insights into advances within feline medicine.<\/jats:p>","DOI":"10.1111\/jvp.13073","type":"journal-article","created":{"date-parts":[[2022,7,5]],"date-time":"2022-07-05T12:51:09Z","timestamp":1657025469000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["The history and pharmacology of buprenorphine: New advances in cats"],"prefix":"10.1111","volume":"45","author":[{"given":"Terrence P.","family":"Clark","sequence":"first","affiliation":[{"name":"Nexcyon Pharmaceuticals, Inc.  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