Bupivacaine HCl (Synonyms: AH 2250, (±)-1-butyl-2′,6′-Pipecoloxylidide)

Cell lines

FDB muscle fibers

Preparation method

The solubility of this compound in DMSO is > 10.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1 mM; 40 mins

Applications

In FDB muscle fibers treated with 1 mM Bupivacaine HCl for 40 mins, the TMRM signal was substantially lost and the fiber shortened significantly. The TMRM signal decreased within about 30 mins, and depolarization was inhibited by CsA, which indicated that Bupivacaine facilitated the opening of the permeability transition pore, eventually causing mitochondrial depolarization.

Animal models

ACLT osteoarthritic rats

Dosage form

0.5%, 10 mL; intra-articular injection; once a week for 5 consecutive weeks

Applications

In ACLT osteoarthritic rats treated with Bupivacaine HCl, the relative weight-bearing values were significantly lower at the 6th and 7th weeks. Besides, Bupivacaine HCl did not show any significant effect on the viability and density of chondrocytes, as well as the histological characteristics of articular cartilage when compared with saline solution injections.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Irwin W, Fontaine E, Agnolucci L, Penzo D, Betto R, Bortolotto S, Reggiani C, Salviati G, Bernardi P. Bupivacaine myotoxicity is mediated by mitochondria. J Biol Chem. 2002 Apr 5;277(14):12221-7.

[2]. Iwasaki K, Sudo H, Kasahara Y, Yamada K, Ohnishi T, Tsujimoto T, Iwasaki N. Effects of Multiple Intra-articular Injections of 0.5% Bupivacaine on Normal and Osteoarthritic Joints in Rats. Arthroscopy. 2016 Oct;32(10):2026-2036.