Big Endothelin-3 (1-41) amide (human) is a precursor molecule of the Endothelin (ET)-3 peptide composing of 41 amino acids [1]. Big Endothelin-3 (1-41) amide can be converted into the mature form by ET converting enzyme, increasing the level of immunoreactive endothelin (IR-ET) in vascular smooth muscle cells (VSMC)[2]. Big Endothelin-3 (1-41) amide has been widely used to regulate the nociceptive behavioral responses of mice[3].
In vitro, Big Endothelin-3 (1-41) amide treatment via intravenous injection at 3nmol/kg within 60min produced a long-lasting hypertensive action in ganglion-blocked anaesthetized rats [4].
References:
[1] Davenport A P, Hyndman K A, Dhaun N, et al. Endothelin[J]. Pharmacological reviews, 2016, 68(2): 357-418.
[2] Tsukahara Y, Matsumura Y, Kuninobu K, et al. Phosphoramidon-sensitive endothelin converting enzyme in cultured vascular smooth muscle cells converts big endothelin-3 to endothelin-3[J]. Life sciences, 1993, 53(6): 465-471.
[3] Raffa R B, Schupsky J J, Jacoby H I. Endothelin-induced nociception in mice: mediation by ETA and ETB receptors[J]. The journal of pharmacology and experimental therapeutics, 1996, 276(2): 647-651.
[4] Matsumura Y, Fujita K, Takaoka M, et al. Big endothelin-3-induced hypertension and its inhibition by phosphoramidon in anaesthetized rats[J]. European journal of pharmacology, 1993, 230(1): 89-93.