Abstract |
AZ002 (L-threo-(3,4-dihydroxy phenyl)-N-methyl serine methyl ester) is a newly synthesized adrenaline derivative. AZ002 caused relaxation of rat jejunum (beta 3-receptors) (ED50 = 18 microM), but did not affect the atrial rate (beta 1) or tracheal relaxation (beta 2) at a concentration of 0.3 mM. The pA2 values for propranolol in inhibiting the isoproterenol- and AZ002-stimulated relaxation of rat jejunum were 6.27 and 6.33, respectively. Thus, AZ002 is a selective agonist for beta 3-adrenoceptor. AZ002 stimulated lipolysis (ED50 = 10 microM) and glucose uptake (ED50 = 1 microM) in rat adipocytes. In both cases, stimulation was antagonized by high concentrations of the beta-adrenoceptor antagonist propranolol, but not by the alpha- adrenoceptor antagonist phentolamine. The effect of AZ002 on glucose uptake was synergistic with that of insulin. AZ002 was also assessed in vivo by using genetically obese mice (KK/Ay strain) with hyperglycemia. Administration of AZ002 in the diet for a week decreased blood glucose and non- esterified fatty acids.
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Authors | Y Hioki, Y Itoh, A Nakajima, T Fukuroda, H Ohasi, T Kamei, M Yano |
Journal | Japanese journal of pharmacology
(Jpn J Pharmacol)
Vol. 69
Issue 3
Pg. 251-8
(Nov 1995)
ISSN: 0021-5198 [Print] Japan |
PMID | 8699633
(Publication Type: Journal Article)
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Chemical References |
- AZ 002
- Glucose
- Epinephrine
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Topics |
- Animals
- Dose-Response Relationship, Drug
- Epinephrine
(analogs & derivatives, pharmacology)
- Glucose
(metabolism)
- Guinea Pigs
- Heart Atria
(drug effects)
- Hypoglycemia
(chemically induced)
- Jejunum
(drug effects)
- Male
- Mice
- Mice, Inbred Strains
- Rats
- Rats, Sprague-Dawley
- Trachea
(drug effects)
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