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

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

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

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

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

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

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

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

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

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

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

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

13                                              Alprenolol inhibited fenoterol-induced beta3-adrenocepto

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

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

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

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