S1319: A novel β2-adrenoceptor agonist from a marine sponge Dysidea sp.

Tracheal relaxing effects and β2 adrenoceptor selectivity of S1319, a novel sponge‐derived bronchodilator agent, in isolated guinea‐pig tissues

“…The concentration‐response curve for S1319 was in parallel with those for isoprenaline, salbutamol and formoterol; it was shifted in a parallel fashion to the right in the presence of β 2 ‐adrenoceptor selective antagonist ICI 118,551 (Figure 3). Furthermore, a radioligand binding experiment using the cell membrane expressing human β 1 ‐ or β 2 ‐adrenoceptor demonstrated that S1319 possessed affinity and selectivity for β 2 ‐adrenoceptor (Suzuki et al ., 1999). These results suggest that S1319 is a β 2 ‐adrenoceptor selective agonist that exerts a potent tracheal relaxing effect.…”

“…Recently, S1319 (4‐hydroxy‐7‐[1‐(1‐hydroxy‐2‐methylamino)ethyl]‐1,3‐benzothiazol‐2(3 H )‐one acetate, Figure 1) has been isolated from marine sponge as a novel bronchodilating agent. Although S1319 does not have a catechol moiety, pharmacological studies have revealed that S1319 possesses binding affinity for β 2 ‐adrenoceptor (Suzuki et al ., 1999).…”

The effects of S1319, a novel marine sponge-derived β 2 -adrenoceptor agonist, on IgE-mediated activation of human cultured mast cells

“…Furthermore, S1319 (Fig. 1), a novel b 2 -selective agonist [22,23], inhibited the tryptase release at the same potency as isoproterenol and formoterol (Fig. 2) and the inhibitory effect of S1319 on the tryptase release was blocked by addition of propranolol (Table 2).…”

“…S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate) (Fig. 1) is a potent b 2 -adrenoceptor agonist with a short duration of action on airways smooth muscle in vitro [22,23]. In the present study, we describe the effect of S1319 (racemate) as an inhibitor of IgE-induced mediator and cytokine release from HCMC, comparing with the non-selective b-adrenoceptor agonist, isoproterenol (R-isomer), the selective b 2 -adrenoceptor agonist, albuterol (racemate), and the selective and long-acting b 2-adrenoceptor agonist, formoterol (racemate).…”

Recent N-Atom Containing Compounds from Indo-Pacific Invertebrates

“…Another benzothiazole derivative designated S1319 was isolated from Dysidea sp. and exhibited bronchodialating activity [15]. …”