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Inhibition of rat colon motility by stimulation of atypical beta-adrenoceptors with new gut-specific agents
- Source :
- Pharmacological Research Communications. 20:147-151
- Publication Year :
- 1988
- Publisher :
- Elsevier BV, 1988.
-
Abstract
- Summary The new putative beta-adrenergic agonists SR 58306A, 2-[(7-hydroxy-1,2,3,4-tetrahydronaphth-2-yl)amino]-1-phenylethanol hydrochloride and SR 58339A, 2-[(7-hydroxy-1,2,3,4-tetrahydronaphth-2-yl)amino]-1-(3-chlorphenyl) ethanol hydrochloride, were studied in vitro in comparison with reference compounds. SR 58306A and SR 58339A, unlike isoprenaline and the beta 2 selective adrenergic agonists salbutamol and ritodrine, potently inhibited rat colon spontaneous contractions (EC 50 5.9 and 1.1×10 −7 M) without increasing guinea-pig atrium frequency or relaxing guinea-pig trachea. The non-selective beta-adrenergic antagonists alprenolol, pindolol and propranolol competitively antagonized the action of SR 58306A on the colon, which was not prevented by either of the selective antagonists atenolol (beta 1 ) and ICI 118551 (beta 2 ). In the same preparation only alprenolol competitively antagonized isoprenaline; antagonism by either pindolol or propranolol was not competitive. These results suggest that in the rat colon isoprenaline interacts with different beta-receptor subclasses, whereas our new gut-specific compounds such as SR 58306A inhibit colonic motility by selectively stimulating atypical beta-adrenoceptors.
- Subjects :
- Male
medicine.medical_specialty
Colon
Adrenergic
Propranolol
In Vitro Techniques
Beta-1 adrenergic receptor
chemistry.chemical_compound
Internal medicine
Isoprenaline
medicine
Animals
Albuterol
Pindolol
Pharmacology
Isoproterenol
Rats, Inbred Strains
Adrenergic beta-Agonists
Atenolol
Rats
Endocrinology
chemistry
Ethanolamines
Ritodrine
Alprenolol
Gastrointestinal Motility
medicine.drug
Subjects
Details
- ISSN :
- 00316989
- Volume :
- 20
- Database :
- OpenAIRE
- Journal :
- Pharmacological Research Communications
- Accession number :
- edsair.doi.dedup.....c89d0a37ccdf1fe9b6301ffa8483231c