1 y slower beta(2)AR off-rates compared to (S)-alprenolol.

2 scribed compound (2.8 A), and the antagonist alprenolol (3.1 A).

3                                        (iii) Alprenolol, a beta-blocker with partial agonist properti

4                    Chronic administration of alprenolol, a beta-blocker without inverse agonist prope

5 ated to CGP12177) and bunitrolol (similar to alprenolol) activated both conformations with biphasic c

6                       Here we show that only alprenolol (Alp) and carvedilol (Car) induce beta(1)AR-m

7 ll antagonists, whereas other ligands [e.g., alprenolol and 1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetra

8 ared as conventional agonists, whereas other alprenolol and bucindolol analogs lost all receptor inte

9 ith [(125)I]IAS was blocked by 10 microM (-)-alprenolol and inhibited by addition of GTP gamma S, and

10 partial agonist (dobutamine), an antagonist (alprenolol), and an inverse agonist (ICI-118,551) to the

11 e CAM beta2-adrenoceptor-expressing cells to alprenolol, and a much smaller effect of betaxolol was p

12 ne, metaproterenol, salmeterol, propranolol, alprenolol, bisoprolol, ICI 118,551, and bucindolol) was

13 cholamine site, whereas others (pindolol and alprenolol) can stimulate both.

14            Very weak partial agonists (e.g., alprenolol) did not increase intracellular cAMP (only st

15 ges in AC activity, with the partial agonist alprenolol increasing (22 +/- 1%) and the inverse agonis

16                                              Alprenolol inhibited fenoterol-induced beta3-adrenocepto

17 igned based on docking of the antagonist (S)-alprenolol into the OBS and an MBS and synthesized.

18 ild-type receptor but not for the antagonist alprenolol or the inverse agonist betaxolol.

19 cted poses CGP12177 and 3 biphasic agonists (alprenolol, oxprenolol, and bucindolol), predictions bas

20 (2)AR in membranes (protectable by 10 microM alprenolol) was demonstrated.

21 nities of antagonists such as propranolol or alprenolol, which have cyclic structures without H-bondi

22 ffinity derivative of the beta AR antagonist alprenolol with a photoactivatable group on the aryloxy