Detail of "105737-62-0"

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Pharmacological characterization of b-adrenoceptor subtypes mediating relaxation in porcine isolated ureteral smooth muscle

Pharmacological characterization of b-adrenoceptor subtypes mediating relaxation in porcine isolated ureteral smooth muscle. Wanajo, Isao; Tomiyama, Yoshitaka; Yamazaki, Yoshinobu; Kojima, Masami; Shibata, Nobuo (Central Research Laboratory, Kissei Pharmaceutical Co., Ltd., Nagano, Japan). Journal of Urology (Hagerstown, MD, United States), 172(3), 1155-1159 (English) 2004 Lippincott Williams & Wilkins. CODEN: JOURAA. ISSN: 0022-5347. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) PURPOSE: We pharmacol. characterized the functional b-adrenoceptor subtypes mediating porcine ureteral smooth muscle relaxation. MATERIALS AND METHODS: The effects of various b-adrenoceptor agonists and antagonists on KCl induced tonic contractions in isolated porcine ureteral prepns.In this article, certain chemicals are used. Some of their cas registry numbers are 51-43-4 and 105737-62-0 were evaluated using a functional exptl. technique. RESULTS: The rank order of potency for the catecholamines tested was isoprenaline > adrenaline > noradrenaline. All b2-adrenoceptor agonists tested (salbutamol, procaterol and terbutaline) attenuated the KCl induced contraction. The 2 b3-adrenoceptor agonists CL-316243 ((R, R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethylamino]propyl]-1,3-benzodiox ole-2,2-dicarboxylate], Kissei, Nagano, Japan) and CGP-12177A ((±)[4-[3[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2 H-benzimidazol-2-one hydrochloride], Funakoshi, Tokyo, Japan) also relaxed the ureter. The b1-adrenoceptor agonist dobutamine had a relaxing effect on the ureter only at high concns. (over 1 ′ 10 M). Isoprenaline induced relaxation was antagonized by the b2-adrenoceptor antagonist ICI-118,551 ((±)-1-[(2,3-dihydro-7-methyl-1 H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride, Sigma, St. Louis, Missouri) but not by the b1-adrenoceptor antagonist CGP 20712A ((±)-2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1 H-imidazol-2-yl]phenoxy]propyl]amino]ethoxy]-benzamide methanesulfonate, Funakoshi). In the presence of 1′ 10 M CGP 20712A plus 1 ′ 10 M ICI-118,551 the b 3-adrenoceptor antagonist SR 58894A (3-(2-allylphenoxy)-1-[(1 S)-1,2,3,4-tetrahydronaphth-1-ylamino]-(2 S)-2-propanol hydrochloride, Kissei) antagonized isoprenaline induced relaxation. CONCLUSIONS: Our results suggest that porcine ureteral smooth muscle is relaxed by b2 and b 3-adrenergic stimulation, as in humans. .

b-Adrenoceptor subtype expression and function in rat white adipocytes

b-Adrenoceptor subtype expression and function in rat white adipocytes. Germack, Renee; Starzec, Anna B.; Vassy, Roger; Perret, Gerard Y. ( Laboratoire de Pharmacologie Clinique et Experimentale, Department de Biophysique et de Pharmacologie des Biosignaux, Faculte de Medicine, Universite Paris-Nord, Bobigny 93017, Fr.). British Journal of Pharmacology, 120(2), 201-210 (English) 1997 Stockton. CODEN: BJPCBM. ISSN: 0007-1188. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The pharmacol. features of rat white adipocyte b-adrenoceptor subtypes were investigated by satn. and b-agonist competition studies with [3H]CGP 12177 and by lipolysis induced by b-agonists as well as their inhibition by CGP 20712A (selective b1-antagonist) and ICI 118551 (selective b2-antagonist) to establish a relation between the functionality and binding capacity of b-adrenoceptor subtypes. Two populations of binding sites were identified on adipocyte membranes, one with high affinity (0.22 nM) and the other with low affinity (23 nM). The low affinity binding sites constituted 90% of the total binding sites. The competition curves, with 15 nM [3H]CGP 12177, for the b-agonists, isoprenaline (Iso), noradrenaline (NA) and adrenaline (Ad), and the selective b3-agonist, BRL 37344 (BRL), were clearly biphasic. The rank orders of agonist potency (pKi) in competing for [3H]CGP 12177 high affinity and low affinity binding sites, resp., were Iso (9.28)>NA (8.90)>Ad (8.65)> > BRL (4.53) and BRL (7.38)> > Iso (2.96)3NA (2.Some commonly used reagents like 105737-62-0 and 34368-04-2 are used in this experiment.80)>Ad (2.10) indicating the expression of b1- and b3-adrenoceptor subtypes on rat white adipocytes, resp. Inversely, competition studies with the selective b1-agonist, xamoterol (Xam), provided evidence for a single homogeneous population of binding sites with low d. (81 fmol mg-1) and high pKi value (7.23) confirming the presence of b1-adrenoceptors. To assess a possible contribution of the b2-subtype, procaterol (Proc), a selective b2-agonist, was used to compete with 2 nM [3H]CGP 12177. A single low affinity (4.61) population of binding sites was identified. The d. of these sites (71 fmol mg-1) was similar to the one obtained with Xam, suggesting that Proc displaced [3H]CGP 12177 from the b1-subtype. The functional potency (pD2) order with BRL (9.07) and catecholamines (Iso: 7.26, NA: 6.89 and Ad: 6.32) was the same as that found for the low affinity binding sites in competition studies. Xam induced lipolysis with greater potency than dobutamine (Dob), 6.31 and 5.66, resp. Proc stimulated lipolysis with a low potency (5.59). The lipolytic response to 0.001 mM BRL was inhibited by both, selective b1- and b2-antagonist, in a monophasic manner with low potencies (CGP 20712A pKi: <4.5 and ICI 118551 pKi: 5.57±0.13). Similar monophasic profiles were obtained for inhibition of Xam- and Dob-induced lipolysis. In this case, CGP 20712A was more potent (> 10 times) than ICI 118551. The monophasic inhibition was also obsd. with ICI 118551 in the presence of 0.05 mM Iso or 0.13 mM NA. In contrast, two populations of sites were identified with CGP 20712A in the presence of Iso as well as NA. The pKi values for the first sites were 8.41 and 8.58, resp., and for the second population of sites 4.73 and 4.27, resp. The proportion of the first sites was low: 19 and 22%, resp. Biphasic curves were obtained with both antagonists using 2.5 mM Proc (CGP 20712A: pKi1: 8.17, site 1: 23%, pKi2: 4.77; ICI 118551: pKi1: 7.78, site 1: 37%, pKi2: 5.35). The results show that the radioligand [3H]CGP 12177 allows the characterization of b1- and b3-adrenoceptor subtypes on rat white adipocytes. Lipolysis is highly dependent on b1- and b3- adrenoceptors. Finally, binding and functional studies confirm that lipolysis is mainly driven by the b3-subtype. .