Carborane Derived Local Anesthetics Show Isomer-Dependent Analgesia

Clinically there is a need for local anesthetics with a greater specificity of action and longer duration. We have synthesized a series of local anesthetic derivatives we call boronicaines in which the aromatic, phenyl ring of lidocaine was replaced with ortho-, meta-, dimethyl meta- and para-carborane clusters. The boronicaine derivatives were tested for their analgesic activity and compared to lidocaine using standard procedures in mice following a plantar injection. The compounds differed in their analgesic activity in the following order: ortho-carborane = dimethyl meta-carborane > para-carborane > lidocaine > meta-carborane derivative. Both

Keywords:

• Internal medicine
• Endocrinology
• Anesthesia
• Biology
• Local anesthetic
• Lidocaine
• Carborane
• Analgesic
• Pharmacology