N-aminoalkylsuccinimides as local anaesthetics. II. 1,2,3,4-Tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-diones substituted in the aromatic nucleus
Sandberg, R.; Domeij, K.E.; Stening, G.; Svensson, S.; Willman, N.; Akerman, B.
Acta Pharmaceutica Suecica 17(4): 169-176
1980
ISSN/ISBN: 0001-6675 PMID: 7468236 Document Number: 155253
In a series of 1'-aminoalkyl-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-diones, substitution in the 7-position by methyl, fluorine, chlorine, hydroxyl, methoxyl or isopropoxyl increased, with few exceptions, the topical anesthetic potency and the i.v. toxicity in animals compared to previously reported unsubstituted compounds. Compounds substituted in the 6-position by methoxyl were less potent and toxic than the corresponding unsubstituted compounds. Some of the new compounds possess a clearly higher surface anesthetic potency than lidocaine and are at least as effective as lidocaine in major nerve blocks.