PMID- 1976401
OWN - NLM
STAT- MEDLINE
DCOM- 19901119
LR  - 20190510
IS  - 0007-1188 (Print)
IS  - 0007-1188 (Linking)
VI  - 100
IP  - 4
DP  - 1990 Aug
TI  - In vitro inhibition of intestinal motility by phenylethanolaminotetralines: 
      evidence of atypical beta-adrenoceptors in rat colon.
PG  - 831-9
AB  - 1. The new compounds phenylethanolaminotetralines (PEAT), unlike the reference 
      beta-adrenoceptor agonists isoprenaline (Iso), ritodrine (Ri) and salbutamol 
      (Sal), produced half-maximal inhibition of spontaneous motility of rat isolated 
      proximal colon at substantially lower concentrations (EC50 2.7-30 nM) than those 
      inducing beta 2-adrenoceptor-mediated responses (relaxation of guinea-pig 
      isolated trachea and rat uterus) and had virtually no chronotropic action (EC50 
      greater than 3 x 10(5) M) on the guinea-pig isolated atrium (a beta 
      1-adrenoceptor-mediated response). 2. The nonselective beta-adrenoceptor 
      antagonists alprenolol and propranolol prevented the inhibition of rat colon 
      motility by the PEAT with low and different potencies (pA2 values around 7.5 and 
      6.5 respectively). Conversely alprenolol and propranolol had a higher and similar 
      potency (pA2 values around 9.0) in preventing typical beta 1 or beta 2-responses 
      (increase in atrial frequency by Iso or tracheal relaxation by Ri or Sal). 3. The 
      selective beta-adrenoceptor antagonists CGP 20712A (beta 1) and ICI 118,551 (beta 
      2) either alone or in combination, did not prevent rat colon motility inhibition 
      by the representative PEAT SR 58611A, which was also fully resistant to 
      alpha-adrenoceptor, acetylcholine, dopamine, histamine, opioid and 
      5-hydroxytryptamine antagonists. 4. These results indicate that the PEAT are a 
      new class of beta-adrenoceptor agonists and suggest that their preferential 
      intestinal action may be accounted for by selectivity for atypical 
      beta-adrenoceptors, abundant in the rat colon and distinct from the currently 
      recognized beta 1 and beta 2 subtypes.
FAU - Bianchetti, A
AU  - Bianchetti A
AD  - Research Center Sanofi-Midy S.p.A., Milan, Italy.
FAU - Manara, L
AU  - Manara L
LA  - eng
PT  - Journal Article
PL  - England
TA  - Br J Pharmacol
JT  - British journal of pharmacology
JID - 7502536
RN  - 0 (Adrenergic beta-Agonists)
RN  - 0 (Adrenergic beta-Antagonists)
RN  - 0 (Ethanolamines)
RN  - 0 (Receptors, Adrenergic, beta)
RN  - 0 (Tetrahydronaphthalenes)
SB  - IM
MH  - Adrenergic beta-Agonists/pharmacology
MH  - Adrenergic beta-Antagonists/pharmacology
MH  - Animals
MH  - Colon/*drug effects
MH  - Ethanolamines/*pharmacology
MH  - Female
MH  - Gastrointestinal Motility/*drug effects
MH  - Guinea Pigs
MH  - In Vitro Techniques
MH  - Male
MH  - Muscle Contraction/drug effects
MH  - Rats
MH  - Rats, Inbred Strains
MH  - Receptors, Adrenergic, beta/*drug effects
MH  - Tetrahydronaphthalenes/*pharmacology
MH  - Trachea/drug effects
MH  - Uterus/drug effects
PMC - PMC1917598
EDAT- 1990/08/01 00:00
MHDA- 1990/08/01 00:01
PMCR- 1991/08/01
CRDT- 1990/08/01 00:00
PHST- 1990/08/01 00:00 [pubmed]
PHST- 1990/08/01 00:01 [medline]
PHST- 1990/08/01 00:00 [entrez]
PHST- 1991/08/01 00:00 [pmc-release]
AID - 10.1111/j.1476-5381.1990.tb14100.x [doi]
PST - ppublish
SO  - Br J Pharmacol. 1990 Aug;100(4):831-9. doi: 10.1111/j.1476-5381.1990.tb14100.x.