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Chemical Compound Review

Semotiadil     (8R)-8-[2-[3-(2- benzo[1,3]dioxol-5...

Synonyms: Semotiadilum, CHEMBL57684, SureCN80715, CHEBI:189474, AC1Q6FJY, ...
 
 
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Disease relevance of Semotiadil

 

High impact information on Semotiadil

  • To identify the binding domain of a new Ca2+ antagonist semotiadil on L-type Ca2+ channels from skeletal muscle, photolabeling was carried out by using an azidophenyl derivative of [3H]semotiadil [6].
  • Efficient identification of photolabelled amino acid residues by combining immunoaffinity purification with MS: revealing the semotiadil-binding site and its relevance to binding sites for myristates in domain III of human serum albumin [7].
  • Human serum albumin (HSA) was photolabelled with an azidophenyl derivative of semotiadil, FNAK [(+)-(R)-3,4-dihydro-2-[5-methoxy-2-[3-[N-methyl-N-[2-(3-azidophenoxy)-ethyl]amino]propoxyl]phenyl]-4-methyl-2H-1,4-benzothiazin-3-(4H)-one], since HSA is a major binding protein for semotiadil in serum [7].
  • Effects of semotiadil fumarate, a novel Ca2+ antagonist, on cytosolic Ca2+ level and force of contraction in porcine coronary arteries [8].
  • Semotiadil even at the higher concentration (10 microM) did not displace specific binding of [3H]-pyrilamine to bovine cerebellar membranes [8].
 

Chemical compound and disease context of Semotiadil

  • Verapamil and semotiadil exhibited a significantly greater effect than diltiazem on the mean ventricular cycle length (VCLmeun), on the maximal ventricular cycle length (VCLmax) and on the standard deviation of the VCL (SD(VCL)) during atrial flutter [4].
  • These results indicate that combined daily dosing of semotiadil, especially with enalapril, each at relatively low doses may be able to control hypertension in a continuous manner [9].
 

Biological context of Semotiadil

 

Anatomical context of Semotiadil

  • The Ca2+ channel blocking compound semotiadil showed the most pronounced rate-dependent effects on the AV node [14].
  • The influence of semotiadil fumarate, a novel vasoselective Ca2+ channel antagonist with a benzothiazine skeleton, was measured on the high-threshold Ca2+ current ICa,L in guinea-pig ventricular myocytes prepared by coronary perfusion with collagenase solution [1].
  • Effects of semotiadil, a novel calcium antagonist, on the retina and optic nerve head circulation [15].
  • These results suggest that semotiadil and SD-3212 inhibit contractions of vascular smooth muscle (VSM) not only through blockade of voltage-dependent Ca2+ channels but also through other mechanisms, such as inhibition of Ca2+ release from Ca2+ stores or decrease in sensitivity of the contractile elements to Ca2+ [16].
  • Effects of semotiadil on the voltage-dependent Ca current (ICa) were investigated in dispersed smooth muscle cells of the rabbit portal vein [17].
 

Associations of Semotiadil with other chemical compounds

 

Gene context of Semotiadil

  • These results indicate that semotiadil may have the strongest antioxidant activity on LDL among the calcium antagonists examined [19].
 

Analytical, diagnostic and therapeutic context of Semotiadil

  • Changes in NB(retina) from the baseline in the semotiadil group was significantly greater than those in the control group 50 min or later after the administration (P < 0.0500, Mann-Whitney test) [15].
  • Twenty-four hours later (day 1), oral administration of semotiadil (10, 30, or 100 mg/kg per day) or diltiazem (100 or 300 mg/kg per day) was initiated [5].

References

  1. A novel benzothiazine Ca2+ channel antagonist, semotiadil, inhibits cardiac L-type Ca2+ currents. Koidl, B., Miyawaki, N., Tritthart, H.A. Eur. J. Pharmacol. (1997) [Pubmed]
  2. Effects of semotiadil fumarate, a novel calcium antagonist, on blood pressure and heart rate in conscious spontaneously hypertensive rats. Kanda, A., Hashimoto, H. Jpn. J. Pharmacol. (1993) [Pubmed]
  3. Effects of semotiadil (SD-3211), a benzothiazine calcium antagonist, on blood pressure and atrioventricular conductivity in anesthetized dogs. Kageyama, M., Yamada, H., Satoh, K., Taira, N. Jpn. J. Pharmacol. (1992) [Pubmed]
  4. Efficacy of the novel calcium antagonist R(+)-semotiadil in limiting the ventricular rate during atrial flutter in isolated guinea pig hearts. Schwarzl, I., Stark, U., Brodmann, M., Haiden, U., Tritthart, H.A., Stark, G. J. Cardiovasc. Pharmacol. (2000) [Pubmed]
  5. Semotiadil inhibits the development of right ventricular hypertrophy and medial thickening of pulmonary arteries in a rat model of pulmonary hypertension. Takahashi, T., Kanda, T., Imai, S., Suzuki, T., Kobayashi, I., Murata, K. Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy. (1995) [Pubmed]
  6. Photochemical identification of transmembrane segment IVS6 as the binding region of semotiadil, a new modulator for the L-type voltage-dependent Ca2+ channel. Kuniyasu, A., Itagaki, K., Shibano, T., Iino, M., Kraft, G., Schwartz, A., Nakayama, H. J. Biol. Chem. (1998) [Pubmed]
  7. Efficient identification of photolabelled amino acid residues by combining immunoaffinity purification with MS: revealing the semotiadil-binding site and its relevance to binding sites for myristates in domain III of human serum albumin. Kawahara, K., Kuniyasu, A., Masuda, K., Ishiguro, M., Nakayama, H. Biochem. J. (2002) [Pubmed]
  8. Effects of semotiadil fumarate, a novel Ca2+ antagonist, on cytosolic Ca2+ level and force of contraction in porcine coronary arteries. Kageyama, M., Yanagisawa, T., Taira, N. Br. J. Pharmacol. (1995) [Pubmed]
  9. Antihypertensive effects of a novel calcium antagonist, semotiadil fumarate (SD-3211), alone and in combination with enalapril or trichlormethiazide in spontaneously hypertensive rats. Ichikawa, M., Wanaka, M., Ohtsuji, T., Akashi, S., Machidera, Y., Manno, K., Nakamuta, H., Koida, M. Biol. Pharm. Bull. (1994) [Pubmed]
  10. Photochemical localization of the semotiadil binding region within the cardiac Ca2+ channel alpha1 subunit. Comparison with the skeletal muscle counterpart. Ii, N., Kuniyasu, A., Kawahara, K., Shibano, T., Schwartz, A., Nakayama, H. FEBS Lett. (1998) [Pubmed]
  11. Effects of semotiadil fumarate (SD-3211) on renal hemodynamics and function in dogs. Nishiyama, A., Tamaki, T., Masumura, H., He, H., Kiyomoto, H., Aki, Y., Yamamoto, A., Iwao, H., Abe, Y. Eur. J. Pharmacol. (1992) [Pubmed]
  12. Quantitative structure-activity relationships of Ca(2+)-antagonistic semotiadil congeners. Fujimura, K., Ota, A., Kawashima, Y. Chem. Pharm. Bull. (1996) [Pubmed]
  13. Antiplatelet activity of semotiadil fumarate. Wolfram, R.M., Kritz, H., Oguogho, A., Sinzinger, H. Thromb. Res. (2002) [Pubmed]
  14. Effects of semotiadil, a novel Ca2+ channel antagonist, on the electrical activity of Langendorff-perfused guinea pig hearts in comparison with diltiazem, amlodipine and nifedipine. Stark, G., Kasper, K., Stark, U., Miyawaki, N., Decrinis, M., Tritthart, H.A. Eur. J. Pharmacol. (1995) [Pubmed]
  15. Effects of semotiadil, a novel calcium antagonist, on the retina and optic nerve head circulation. Tomita, K., Tomidokoro, A., Tamaki, Y., Araie, M., Matsubara, M., Fukaya, Y. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics. (2000) [Pubmed]
  16. Effects of semotiadil fumarate (SD-3211) and its enantiomer, SD-3212, on the changes in cytosolic Ca2+ and tension caused by KCl and norepinephrine in isolated rat aortas. Murakami, K., Shindo, K., Ito, K.M., Ito, K. J. Cardiovasc. Pharmacol. (1995) [Pubmed]
  17. Mechanisms of the inhibitory action of semotiadil fumarate, a novel Ca antagonist, on the voltage-dependent Ca current in smooth muscle cells of the rabbit portal vein. Teramoto, N. Jpn. J. Pharmacol. (1993) [Pubmed]
  18. Enantioselective local disposition of semotiadil (R-enantiomer) and levosemotiadil (S-enantiomer) in perfused rat liver. Ueda, K., Yamaoka, K., Rodriguez, M.E., Shibukawa, A., Nakagawa, T. Drug Metab. Dispos. (1997) [Pubmed]
  19. Semotiadil, a new calcium antagonist, is a very potent inhibitor of LDL-oxidation. Kritz, H., Oguogho, A., Aghajanian, A.A., Sinzinger, H. Prostaglandins Leukot. Essent. Fatty Acids (1999) [Pubmed]
 
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