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Hiromi Fukamachi - One of the best experts on this subject based on the ideXlab platform.
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Tracheal relaxing effects and β2 adrenoceptor selectivity of S1319, a novel sponge-derived bronchodilator Agent, in isolated guinea-pig tissues
British journal of pharmacology, 1999Co-Authors: Hidefumi Suzuki, Akihiro Ueno, Masao Takei, Kazutoshi Sindo, Toru Miura, Masayuki Sakakibara, Tatsuo Higa, Hiromi FukamachiAbstract:S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate), a novel non-catecholamine β-adrenoceptor agonist, has been compared with isoprenaline, salbutamol and formoterol for activity in vitro on a range of β-adrenoceptor containing preparations from guinea-pig. S1319, like isoprenaline, salbutamol and formoterol, relaxed preparations of guinea-pig trachea (contracted by histamine) in a concentration-dependent manner. The relaxing activity of S1319 appeared to be more potent than that of isoprenaline and salbutamol, and similar to that of formoterol (pD2 values of 10.58±0.03 vs 7.60±0.01, 7.50±0.01 and 10.52±0.04, respectively), and was blocked by the β2-adrenoceptor selective antagonist (ICI 118,551). The intrinsic activity of S1319 was close to 1.0. In the β1-adrenoceptor containing preparations, guinea-pig right and left atria, a monophasic inotropic response of S1319 was observed. The pD2 value of S1319 for left atrial and right atrial inotropism was 6.70±0.15 and 7.81±0.01, respectively. The selectivity ratio (trachea/left atrial inotropism) of S1319, formoterol, salbutamol and isoprenaline was 8523, 284, 4.8 and 0.45, respectively. The relative selectivity ratio of S1319 was 18743, 1858 and 30 times greater than that of isoprenaline, salbutamol and formoterol, respectively. Relaxant responses of guinea-pig trachea to S1319 declined rapidly when the agonist was washed from the tissues, with complete recovery within 30 min. The duration of action of S1319 was similar to that of isoprenaline and less than that of salbutamol and formoterol. In summary, S1319, a sponge-derived β-adrenoceptor agonist, is a potent and selective β2-adrenoceptor agonist with a short-duration of action in isolated guinea-pig tracheas. Keywords: β2-Adrenoceptor agonist, tracheal smooth muscle relaxation, duration of action Introduction β2-Adrenoceptor agonists form an important class of therapeutic Agents in asthma. Selective β2-adrenoceptor agonists are clinically the most widely used and effective bronchodilators because they have low cardiac side effects. Historically, isoprenaline has been the most popular β-adrenoceptor stimulant but it has some disadvantages such as tachycardia due to its low selectivity towards the airway. Consequently, many bronchodilators such as trimetoquinol (Sato et al., 1980), salbutamol (O'Donnell, 1972; Cullum et al., 1969), procaterol (Yabuuchi, 1977), formoterol (Ida, 1976), salmeterol (Ball et al., 1987a,1987b; 1991; Bradshaw et al., 1987), TA-2005 (Kikkawa et al., 1991; Voss et al., 1992; 1994) which are selective for bronchial smooth muscle, have been developed. Recently, S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate, Figure 1) has been isolated from marine sponge as a novel Bronchodilating Agent. Although S1319 does not have a catechol moiety, pharmacological studies have revealed that S1319 possesses binding affinity for β2-adrenoceptor (Suzuki et al., 1999). Figure 1 Chemical structure of S1319. In the present study, we investigated the tracheal relaxing effect and β2-selectivity of S1319 in guinea-pigs by pharmacological studies to characterize its properties. The effects of S1319 were also compared with those of other β-adrenoceptor agonists, salbutamol, formoterol and isoprenaline. It was found that S1319 exhibited much more β2-selectivity than the other compounds tested and had a short duration of action.
Jim M. Wild - One of the best experts on this subject based on the ideXlab platform.
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Regional ventilation changes in the lung: Treatment response mapping by using hyperpolarized gas MR imaging as a quantitative biomarker
Radiology, 2017Co-Authors: Felix Horn, Helen Marshall, Guilhem Collier, Richard Kay, Salman Siddiqui, Christopher E. Brightling, Juan Parra-robles, Jim M. WildAbstract:Purpose To assess the magnitude of regional response to respiratory therapeutic Agents in the lungs by using treatment response mapping (TRM) with hyperpolarized gas magnetic resonance (MR) imaging. TRM was used to quantify regional physiologic response in adults with asthma who underwent a bronchodilator challenge. Materials and Methods This study was approved by the national research ethics committee and was performed with informed consent. Imaging was performed in 20 adult patients with asthma by using hyperpolarized helium 3 (3He) ventilation MR imaging. Two sets of baseline images were acquired before inhalation of a Bronchodilating Agent (salbutamol 400 μg), and one set was acquired after. All images were registered for voxelwise comparison. Regional treatment response, ΔR(r), was calculated as the difference in regional gas distribution (R[r] = ratio of inhaled gas to total volume of a voxel when normalized for lung inflation volume) before and after intervention. A voxelwise activation threshold from the variability of the baseline images was applied to ΔR(r) maps. The summed global treatment response map (ΔRnet) was then used as a global lung index for comparison with metrics of bronchodilator response measured by using spirometry and the global imaging metric percentage ventilated volume (%VV). Results ΔRnet showed significant correlation (P < .01) with changes in forced expiratory volume in 1 second (r = 0.70), forced vital capacity (r = 0.84), and %VV (r = 0.56). A significant (P < .01) positive treatment effect was detected with all metrics; however, ΔRnet showed a lower intersubject coefficient of variation (64%) than all of the other tests (coefficient of variation, ≥99%). Conclusion TRM provides regional quantitative information on changes in inhaled gas ventilation in response to therapy. This method could be used as a sensitive regional outcome metric for novel respiratory interventions. © RSNA, 2017 Online supplemental material is available for this article.
Hidefumi Suzuki - One of the best experts on this subject based on the ideXlab platform.
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Tracheal relaxing effects and β2 adrenoceptor selectivity of S1319, a novel sponge-derived bronchodilator Agent, in isolated guinea-pig tissues
British journal of pharmacology, 1999Co-Authors: Hidefumi Suzuki, Akihiro Ueno, Masao Takei, Kazutoshi Sindo, Toru Miura, Masayuki Sakakibara, Tatsuo Higa, Hiromi FukamachiAbstract:S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate), a novel non-catecholamine β-adrenoceptor agonist, has been compared with isoprenaline, salbutamol and formoterol for activity in vitro on a range of β-adrenoceptor containing preparations from guinea-pig. S1319, like isoprenaline, salbutamol and formoterol, relaxed preparations of guinea-pig trachea (contracted by histamine) in a concentration-dependent manner. The relaxing activity of S1319 appeared to be more potent than that of isoprenaline and salbutamol, and similar to that of formoterol (pD2 values of 10.58±0.03 vs 7.60±0.01, 7.50±0.01 and 10.52±0.04, respectively), and was blocked by the β2-adrenoceptor selective antagonist (ICI 118,551). The intrinsic activity of S1319 was close to 1.0. In the β1-adrenoceptor containing preparations, guinea-pig right and left atria, a monophasic inotropic response of S1319 was observed. The pD2 value of S1319 for left atrial and right atrial inotropism was 6.70±0.15 and 7.81±0.01, respectively. The selectivity ratio (trachea/left atrial inotropism) of S1319, formoterol, salbutamol and isoprenaline was 8523, 284, 4.8 and 0.45, respectively. The relative selectivity ratio of S1319 was 18743, 1858 and 30 times greater than that of isoprenaline, salbutamol and formoterol, respectively. Relaxant responses of guinea-pig trachea to S1319 declined rapidly when the agonist was washed from the tissues, with complete recovery within 30 min. The duration of action of S1319 was similar to that of isoprenaline and less than that of salbutamol and formoterol. In summary, S1319, a sponge-derived β-adrenoceptor agonist, is a potent and selective β2-adrenoceptor agonist with a short-duration of action in isolated guinea-pig tracheas. Keywords: β2-Adrenoceptor agonist, tracheal smooth muscle relaxation, duration of action Introduction β2-Adrenoceptor agonists form an important class of therapeutic Agents in asthma. Selective β2-adrenoceptor agonists are clinically the most widely used and effective bronchodilators because they have low cardiac side effects. Historically, isoprenaline has been the most popular β-adrenoceptor stimulant but it has some disadvantages such as tachycardia due to its low selectivity towards the airway. Consequently, many bronchodilators such as trimetoquinol (Sato et al., 1980), salbutamol (O'Donnell, 1972; Cullum et al., 1969), procaterol (Yabuuchi, 1977), formoterol (Ida, 1976), salmeterol (Ball et al., 1987a,1987b; 1991; Bradshaw et al., 1987), TA-2005 (Kikkawa et al., 1991; Voss et al., 1992; 1994) which are selective for bronchial smooth muscle, have been developed. Recently, S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate, Figure 1) has been isolated from marine sponge as a novel Bronchodilating Agent. Although S1319 does not have a catechol moiety, pharmacological studies have revealed that S1319 possesses binding affinity for β2-adrenoceptor (Suzuki et al., 1999). Figure 1 Chemical structure of S1319. In the present study, we investigated the tracheal relaxing effect and β2-selectivity of S1319 in guinea-pigs by pharmacological studies to characterize its properties. The effects of S1319 were also compared with those of other β-adrenoceptor agonists, salbutamol, formoterol and isoprenaline. It was found that S1319 exhibited much more β2-selectivity than the other compounds tested and had a short duration of action.
Masao Takei - One of the best experts on this subject based on the ideXlab platform.
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Tracheal relaxing effects and β2 adrenoceptor selectivity of S1319, a novel sponge-derived bronchodilator Agent, in isolated guinea-pig tissues
British journal of pharmacology, 1999Co-Authors: Hidefumi Suzuki, Akihiro Ueno, Masao Takei, Kazutoshi Sindo, Toru Miura, Masayuki Sakakibara, Tatsuo Higa, Hiromi FukamachiAbstract:S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate), a novel non-catecholamine β-adrenoceptor agonist, has been compared with isoprenaline, salbutamol and formoterol for activity in vitro on a range of β-adrenoceptor containing preparations from guinea-pig. S1319, like isoprenaline, salbutamol and formoterol, relaxed preparations of guinea-pig trachea (contracted by histamine) in a concentration-dependent manner. The relaxing activity of S1319 appeared to be more potent than that of isoprenaline and salbutamol, and similar to that of formoterol (pD2 values of 10.58±0.03 vs 7.60±0.01, 7.50±0.01 and 10.52±0.04, respectively), and was blocked by the β2-adrenoceptor selective antagonist (ICI 118,551). The intrinsic activity of S1319 was close to 1.0. In the β1-adrenoceptor containing preparations, guinea-pig right and left atria, a monophasic inotropic response of S1319 was observed. The pD2 value of S1319 for left atrial and right atrial inotropism was 6.70±0.15 and 7.81±0.01, respectively. The selectivity ratio (trachea/left atrial inotropism) of S1319, formoterol, salbutamol and isoprenaline was 8523, 284, 4.8 and 0.45, respectively. The relative selectivity ratio of S1319 was 18743, 1858 and 30 times greater than that of isoprenaline, salbutamol and formoterol, respectively. Relaxant responses of guinea-pig trachea to S1319 declined rapidly when the agonist was washed from the tissues, with complete recovery within 30 min. The duration of action of S1319 was similar to that of isoprenaline and less than that of salbutamol and formoterol. In summary, S1319, a sponge-derived β-adrenoceptor agonist, is a potent and selective β2-adrenoceptor agonist with a short-duration of action in isolated guinea-pig tracheas. Keywords: β2-Adrenoceptor agonist, tracheal smooth muscle relaxation, duration of action Introduction β2-Adrenoceptor agonists form an important class of therapeutic Agents in asthma. Selective β2-adrenoceptor agonists are clinically the most widely used and effective bronchodilators because they have low cardiac side effects. Historically, isoprenaline has been the most popular β-adrenoceptor stimulant but it has some disadvantages such as tachycardia due to its low selectivity towards the airway. Consequently, many bronchodilators such as trimetoquinol (Sato et al., 1980), salbutamol (O'Donnell, 1972; Cullum et al., 1969), procaterol (Yabuuchi, 1977), formoterol (Ida, 1976), salmeterol (Ball et al., 1987a,1987b; 1991; Bradshaw et al., 1987), TA-2005 (Kikkawa et al., 1991; Voss et al., 1992; 1994) which are selective for bronchial smooth muscle, have been developed. Recently, S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate, Figure 1) has been isolated from marine sponge as a novel Bronchodilating Agent. Although S1319 does not have a catechol moiety, pharmacological studies have revealed that S1319 possesses binding affinity for β2-adrenoceptor (Suzuki et al., 1999). Figure 1 Chemical structure of S1319. In the present study, we investigated the tracheal relaxing effect and β2-selectivity of S1319 in guinea-pigs by pharmacological studies to characterize its properties. The effects of S1319 were also compared with those of other β-adrenoceptor agonists, salbutamol, formoterol and isoprenaline. It was found that S1319 exhibited much more β2-selectivity than the other compounds tested and had a short duration of action.
Kazutoshi Sindo - One of the best experts on this subject based on the ideXlab platform.
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Tracheal relaxing effects and β2 adrenoceptor selectivity of S1319, a novel sponge-derived bronchodilator Agent, in isolated guinea-pig tissues
British journal of pharmacology, 1999Co-Authors: Hidefumi Suzuki, Akihiro Ueno, Masao Takei, Kazutoshi Sindo, Toru Miura, Masayuki Sakakibara, Tatsuo Higa, Hiromi FukamachiAbstract:S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate), a novel non-catecholamine β-adrenoceptor agonist, has been compared with isoprenaline, salbutamol and formoterol for activity in vitro on a range of β-adrenoceptor containing preparations from guinea-pig. S1319, like isoprenaline, salbutamol and formoterol, relaxed preparations of guinea-pig trachea (contracted by histamine) in a concentration-dependent manner. The relaxing activity of S1319 appeared to be more potent than that of isoprenaline and salbutamol, and similar to that of formoterol (pD2 values of 10.58±0.03 vs 7.60±0.01, 7.50±0.01 and 10.52±0.04, respectively), and was blocked by the β2-adrenoceptor selective antagonist (ICI 118,551). The intrinsic activity of S1319 was close to 1.0. In the β1-adrenoceptor containing preparations, guinea-pig right and left atria, a monophasic inotropic response of S1319 was observed. The pD2 value of S1319 for left atrial and right atrial inotropism was 6.70±0.15 and 7.81±0.01, respectively. The selectivity ratio (trachea/left atrial inotropism) of S1319, formoterol, salbutamol and isoprenaline was 8523, 284, 4.8 and 0.45, respectively. The relative selectivity ratio of S1319 was 18743, 1858 and 30 times greater than that of isoprenaline, salbutamol and formoterol, respectively. Relaxant responses of guinea-pig trachea to S1319 declined rapidly when the agonist was washed from the tissues, with complete recovery within 30 min. The duration of action of S1319 was similar to that of isoprenaline and less than that of salbutamol and formoterol. In summary, S1319, a sponge-derived β-adrenoceptor agonist, is a potent and selective β2-adrenoceptor agonist with a short-duration of action in isolated guinea-pig tracheas. Keywords: β2-Adrenoceptor agonist, tracheal smooth muscle relaxation, duration of action Introduction β2-Adrenoceptor agonists form an important class of therapeutic Agents in asthma. Selective β2-adrenoceptor agonists are clinically the most widely used and effective bronchodilators because they have low cardiac side effects. Historically, isoprenaline has been the most popular β-adrenoceptor stimulant but it has some disadvantages such as tachycardia due to its low selectivity towards the airway. Consequently, many bronchodilators such as trimetoquinol (Sato et al., 1980), salbutamol (O'Donnell, 1972; Cullum et al., 1969), procaterol (Yabuuchi, 1977), formoterol (Ida, 1976), salmeterol (Ball et al., 1987a,1987b; 1991; Bradshaw et al., 1987), TA-2005 (Kikkawa et al., 1991; Voss et al., 1992; 1994) which are selective for bronchial smooth muscle, have been developed. Recently, S1319 (4-hydroxy-7-[1-(1-hydroxy-2-methylamino)ethyl]-1,3-benzothiazol-2(3H)-one acetate, Figure 1) has been isolated from marine sponge as a novel Bronchodilating Agent. Although S1319 does not have a catechol moiety, pharmacological studies have revealed that S1319 possesses binding affinity for β2-adrenoceptor (Suzuki et al., 1999). Figure 1 Chemical structure of S1319. In the present study, we investigated the tracheal relaxing effect and β2-selectivity of S1319 in guinea-pigs by pharmacological studies to characterize its properties. The effects of S1319 were also compared with those of other β-adrenoceptor agonists, salbutamol, formoterol and isoprenaline. It was found that S1319 exhibited much more β2-selectivity than the other compounds tested and had a short duration of action.
