Anticoccidial activities of 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine and other alpha 2 adrenergic agonists.
نویسندگان
چکیده
Activity against the coccidial pathogen Eimeria tenella in chickens has been discovered among alpha 2 adrenergic agonists. The clonidine analog 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine was active in feed at 7.5 ppm, a concentration similar to the use levels of potent commercial agents, e.g., maduramicin. Additional alpha 2 agonists were also found to have anticoccidial activity, for example, the catecholamine nordefrin, which is chemically unrelated to clonidine. However, alpha 1 agonists and alpha antagonists were inactive. These observations imply that anticoccidial effects reflect involvement of a receptor with the characteristics of the vertebrate alpha 2 adrenoceptor. alpha 2 agonists that permeate the blood-brain barrier (like clonidine) inhibit feed intake at efficacious levels, whereas those that are restricted to the peripheral compartment (such as catecholamines) do not inhibit feed intake as much. Hence, anticoccidial efficacy may be a peripheral adrenergic effect whereas depression of feed intake is likely centrally mediated.
منابع مشابه
Discovery and Characterization of Novel GPR39 Agonists Allosterically Modulated by Zinc.
In this study, we identified two previously described kinase inhibitors-3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine (LY2784544) and 1H-benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)- (GSK2636771)-as novel GPR39 agonists by unbiased small-molecule-based screening ...
متن کامل3-Bromopyrazolo[3,4-d]pyrimidine 2'-deoxy-2'-fluoro-beta-D-arabinonucleosides: modified DNA constituents with an unusually rigid sugar N-conformation.
The nucleobase anion glycosylation of 3-bromo-4-isopropoxy-1H-pyrazolo[3,4-d]pyrimidin-6-amine (6) with 3,5-di-O-benzoyl-2-deoxy-2-fluoro-alpha-d-arabinofuranosyl bromide (5) furnished the protected N(1)-beta-d-nucleosides 7 (60%) and 8 (ca. 2%) along with the N(2)-beta-d-regioisomer 9 (9%). Debenzoylation of compounds 7 and 9 yielded the nucleosides 10 (81%) and 11 (76%). Compound 10 was trans...
متن کاملNovel synthesis of Pyrimido[4,5- e] [1,3,4] thiadiazines
Treatment of 1-(5-bromo-2-chloro-6-methylpyrimidin-4-yl)-1-methylhydrazine with dimethylthiocarbamoylchloride gave 7-chloro-N,N,1,5-tetramethyl-1H-pyrimido[4,5-e][1,3,4]thiadiazin-3-amine in basic acetonitrile. The latter compounds were reacted with secondary amines in boiling ethanol to afford the related 7-amino derivatives.
متن کاملNovel synthesis of Pyrimido[4,5- e] [1,3,4] thiadiazines
Treatment of 1-(5-bromo-2-chloro-6-methylpyrimidin-4-yl)-1-methylhydrazine with dimethylthiocarbamoylchloride gave 7-chloro-N,N,1,5-tetramethyl-1H-pyrimido[4,5-e][1,3,4]thiadiazin-3-amine in basic acetonitrile. The latter compounds were reacted with secondary amines in boiling ethanol to afford the related 7-amino derivatives.
متن کاملDopamine agonist-induced yawning in rats: a dopamine D3 receptor-mediated behavior.
A specific role for the dopamine D3 receptor in behavior has yet to be elucidated. We now report that dopamine D2/D3 agonists elicit dose-dependent yawning behavior in rats, resulting in an inverted U-shaped dose-response curve. A series of experiments was directed toward the hypothesis that the induction of yawning is a D3 receptor-mediated effect, whereas the inhibition of the yawning observe...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Antimicrobial agents and chemotherapy
دوره 36 2 شماره
صفحات -
تاریخ انتشار 1992