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Differentiation of binding sites of CGP12177 and carteolol to the beta-adrenoceptors in guinea-pig taenia caecum


, : Differentiation of binding sites of CGP12177 and carteolol to the beta-adrenoceptors in guinea-pig taenia caecum. Japanese Journal of Pharmacology 71(SUPPL 1): 115P



Accession: 030940234

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Related references

Koike, K.; Takayanagi, I.; Yamazaki, M., 1996: Differentiation of binding sites of CGP12177, a beta 3-adrenoceptor partial agonist, and carteolol, a beta 1/beta 2-adrenoceptor partial agonist, to the beta-adrenoceptors in guinea-pig taenia caecum. Differentiation of binding sites of CGP12177 and carteolol to the beta-adrenoceptors in the guinea-pig taenia caecum was investigated. Carteolol and CGP12177 competitively antagonized the relaxation responses to isoprenaline, and the pA2 values we...

Koike, K.; Takayanagi, I., 1997: Characteristics of [3H]CGP12177 binding sites at beta 2- and beta 3-adrenoceptors in the guinea pig taenia caecum. 1. Experiments were carried out to characterize the [3H]CGP12177 binding sites in the microsomal fraction from the guinea pig taenia caecum. 2. The Scatchard plot in the absence of butoxamine (10(-4) M) or bupranolol (10(-4) M) was concave, sugges...

Koike, K.; Takayanagi, I., 1997: Characteristics of (3H)CGP12177 binding sites at beta-2- and beta-3-adrenoceptors in the guinea pig taenia caecum. 1. Experiments were carried out to characterize the (3H)CGP12177 binding sites in the microsomal fraction from the guinea pig taenia caecum. 2. The Scatchard plot in the absence of butoxamine (10-4 M) or bupranolol (10-4 M) was concave, suggesting...

Takayanagi, I.; Ogishima, M.; Koike, K., 1990: Thermodynamic analysis of beta-adrenergic partial agonists (befunolol and carteolol) interaction with low and high affinity binding sites of beta-adrenoceptors in guinea-pig taenia caecum. 1. Effects of temperatures (0, 10 and 32 degrees C) on the bindings of beta-adrenergic partial agonists, befunolol and carteolol, with beta-adrenoceptors were studied using the microsomal fractions from the guinea-pig taenia caecum. 2. The affinit...

Horinouchi, T.; Koike, K., 2001: Further evidence that (+/-)-carteolol-induced relaxation is mediated by beta2-adrenoceptors but not by beta3-adrenoceptors in the guinea pig taenia caecum. The properties of the beta1- and beta2-adrenoceptor partial agonist (+/-)-carteolol were investigated against the beta2- and beta3-adrenoceptors of the taenia caecum of the guinea pig. (--)-Isoprenaline and (+/-)-carteolol induced concentration-de...

Takayanagi, I.; Koike, K.; Ogishima, M., 1989: Interactions of R(+) and S(-) isomers of befunolol, a partial agonist with high and low affinity sites of beta-adrenoceptors in guinea-pig taenia caecum. The beta-adrenomimetic and beta-adrenolytic activities of R(+) and S(-) isomers of befunolol, a beta-adrenergic partial agonist, were studied in the guinea-pig taenia caecum. The pA2 value (9.38) of the S(-) isomer against S(-) isoprenaline was si...

Takayanagi, I.; Hagiwara, H.; Koike, K., 1990: Stereoselectivity in beta-adrenomimetic and beta-adrenolytic actions of carteolol, a beta-adrenoceptor blocker with intrinsic sympathomimetic action in guinea-pig taenia caecum. 1. The beta-adrenomimetic and beta-adrenolytic activities of S(-) and R(+) isomers of carteolol, a beta-adrenergic partial agonist (a beta-adrenoceptor blocker with intrinsic sympathomimetic action) were tested in the guinea-pig taenia caecum. 2....

Takayanagi, I.; Koike, K., 1983: A possible mechanism of action of a beta-adrenergic partial agonist (carteolol) in guinea pig taenia caecum. Carteolol, 5-(3-tert-butylamino-2-hydroxy)propoxy-3, 4-dihydrocarbostyril hydrochloride was found to be a beta-adrenergic partial agonist in the taenia caecum of guinea pig. Concentration response curves of carteolol and isoprenaline were parallel...

Koike, K.; Takayanagi, I., 1985: A possible mechanism in interaction of a partial agonist with beta-adrenoceptor in guinea-pig taenia caecum: effects of Gpp(NH)p on its two different binding sites. The mechanisms of the actions of the beta-adrenergic partial agonist (befunolol) were studied in isolated guinea-pig taenia caecum. Befunolol, 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran hydrochloride was found to be a typical partial...

Joseph, S.S.; Lynham, J.A.; Colledge, W.H.; Kaumann, A.J., 2004: Binding of (-)-[3H]-CGP12177 at two sites in recombinant human beta 1-adrenoceptors and interaction with beta-blockers. To verify the hypothesis that the non-conventional partial agonist (-)-CGP12177 binds at two beta(1)-adrenoceptor sites, human beta(1)-adrenoceptors, expressed in CHO cells, were labelled with (-)-[(3)H]-CGP12177. We compared the binding affinity...