PMID- 6093567
OWN - NLM
STAT- MEDLINE
DCOM- 19841219
LR  - 20171213
IS  - 0002-9513 (Print)
IS  - 0002-9513 (Linking)
VI  - 247
IP  - 5 Pt 1
DP  - 1984 Nov
TI  - Characterization of a beta-adrenergic receptor in porcine trachealis muscle.
PG  - C342-9
AB  - To establish a model of airway smooth muscle function we studied binding of 
      [3H]dihydroalprenolol [( 3H]DHA), a beta-adrenergic antagonist, to membrane 
      preparations of porcine trachealis muscle and investigated the response of 
      adenylate cyclase to l-isoproterenol in tissue and plasma membranes. [3H]DHA 
      binding was of high affinity (Kd = 1.0 +/- 0.1 nM), was saturable (Bmax = 87.6 
      +/- 13.2 fmol/mg protein), and was 90% beta 2 and 10% beta 1. Adenylate cyclase 
      activity in the membrane preparation was (in pmol.10 min-1.mg protein-1 +/- SE): 
      basal 420 +/- 74, guanosine 5'-triphosphate (GTP) (10 micron) 600 +/- 45, GTP (10 
      microM) + l-isoproterenol (100 microM) 660 +/- 63, NaF (10 mM) 1,500 +/- 134, and 
      forskolin (100 microM) 3,000 +/- 410. Guanosine 5'-diphosphate (GDP) and GTP were 
      active cofactors; l-isoproterenol appeared to function as an effector exchanging 
      GTP for GDP on the guanine nucleotide regulatory protein. There was close 
      agreement of the effective dose (ED50) of the l-isoproterenol-induced relaxation 
      (0.95 +/- 0.45 microM) and the inhibitory constant of l-isoproterenol binding 
      (0.39 +/- 0.10 microM). l-Isoproterenol (100 microM) induced a 100% increase in 
      adenosine 3',5'-cyclic monophosphate (cAMP) levels in tissue strips over basal 
      activity. Investigation of the difference in adenylate cyclase activity between 
      tissue and plasma membranes revealed that l-isoproterenol responsive adenylate 
      cyclase was diminished after initial homogenization. Electron microscopy 
      demonstrated disruption of all cells at this early stage of preparation. The 
      decrease in l-isoproterenol responsive adenylate cyclase following cell rupture 
      is different from other tissues and suggests a difference in the actions of 
      beta-agonist in smooth muscle compared with other tissues.
FAU - Popovich, K J
AU  - Popovich KJ
FAU - Hiller, C
AU  - Hiller C
FAU - Hough, A
AU  - Hough A
FAU - Norris, J S
AU  - Norris JS
FAU - Cornett, L E
AU  - Cornett LE
LA  - eng
GR  - AM-27450/AM/NIADDK NIH HHS/United States
GR  - HL-06617/HL/NHLBI NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - Am J Physiol
JT  - The American journal of physiology
JID - 0370511
RN  - 0 (Receptors, Adrenergic, beta)
RN  - 60106-89-0 (Dihydroalprenolol)
RN  - 85-32-5 (Guanosine Monophosphate)
RN  - 86-01-1 (Guanosine Triphosphate)
RN  - E0399OZS9N (Cyclic AMP)
RN  - EC 3.6.1.- (GTP-Binding Proteins)
RN  - EC 4.6.1.1 (Adenylyl Cyclases)
RN  - L628TT009W (Isoproterenol)
SB  - IM
MH  - Adenylyl Cyclases/metabolism
MH  - Animals
MH  - Cell Membrane/metabolism
MH  - Cyclic AMP/metabolism
MH  - Dihydroalprenolol/pharmacology
MH  - GTP-Binding Proteins/metabolism
MH  - Guanosine Monophosphate/metabolism
MH  - Guanosine Triphosphate/metabolism
MH  - Isoproterenol/pharmacology
MH  - Microscopy, Electron
MH  - Muscle Contraction/drug effects
MH  - Muscle, Smooth/drug effects/*metabolism
MH  - Receptors, Adrenergic, beta/drug effects/*metabolism
MH  - Stimulation, Chemical
MH  - Swine
MH  - Trachea/*metabolism
EDAT- 1984/11/01 00:00
MHDA- 1984/11/01 00:01
CRDT- 1984/11/01 00:00
PHST- 1984/11/01 00:00 [pubmed]
PHST- 1984/11/01 00:01 [medline]
PHST- 1984/11/01 00:00 [entrez]
AID - 10.1152/ajpcell.1984.247.5.C342 [doi]
PST - ppublish
SO  - Am J Physiol. 1984 Nov;247(5 Pt 1):C342-9. doi: 10.1152/ajpcell.1984.247.5.C342.