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Chemical Compound Review

Lopac-U-101     6-[3-[4-(2- methoxyphenyl)piperazin-1...

Synonyms: CHEMBL420060, SureCN6375436, CHEBI:246114, CCG-205348, U-101, ...
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Disease relevance of Lopac-U-101


High impact information on Lopac-U-101


Biological context of Lopac-U-101

  • 5-Methylurapidil, but not the other compounds, recognized binding sites in these cells with a substantially lower affinity than has been observed for the low affinity site in other tissues and in parallel studies with renal cortical membranes [7].
  • The selective antagonists (+)-niguldipine and 5-methylurapidil (5-MU) were used to more clearly identify the alpha 1-adrenergic receptor subtypes involved in second messenger responses in slice and culture preparations of rat brain [8].
  • The difference in inotropy could be blocked by the selective alpha(1A)-AR antagonist, 5-methylurapidil, which correlated with decreases in alpha(1A)-AR density, suggesting that the alpha(1B)-AR had caused a compensatory downregulation of the alpha(1A)-AR [9].
  • Prior blockade of 5-HT1A receptors at this site with bilateral application of spiperone (30 micrograms/side) prevented the hypotensive effect of 5-methyl-urapidil (mean blood pressure now increased by 5 +/- 4 mm Hg) [10].
  • The alpha 1A-selective adrenoceptor antagonist, 5-methylurapidil, inhibited responses to field stimulation in the absence and presence of nifedipine (10 microM) with -log molar (p) IC50 (+/- s.e. mean) values of 7.95 +/- 0.14 and 7.01 +/- 0.07, respectively [11].

Anatomical context of Lopac-U-101


Associations of Lopac-U-101 with other chemical compounds

  • Radioligand binding studies with the nonselective alpha 1-adrenoceptor antagonist radioligand 125I-BE2254 showed that 73-87% of the binding sites in rabbit aorta are CEC sensitive and they are predominantly low affinity sites both for WB4101 (pKd = 8.1) and for 5-methylurapidil (pKd = 7.1) [16].
  • In CEC-pretreated membranes, prazosin, WB4101, 5-methylurapidil and HV723 antagonized the [3H]-prazosin (100 pM) binding monophasically (pKi = 9.70, 9.56, 8.60 and 8.82, for each antagonist) [17].
  • Prazosin (nonselective alpha1 antagonist), 5-methyl urapidil (alpha1A-selective), and BMY 7378 (alpha1D-selective) displaced [3H]prazosin binding curves in caput and cauda epididymis from 40- and 120-day-old rats [18].
  • 2. In prostatic portions of rat vas deferens, the competitive antagonists (-)-discretamine, 5-methylurapidil (5-MU) and prazosin inhibited contractions to noradrenaline (NA) with pA2 values of 6.21, 8.71 and 9.27, respectively [19].
  • 6. It is concluded that the hypotensive agents flesinoxan and 5-methyl-urapidil appear to have different efficacies at 5-HT1A receptors located in different regions of the rodent brain [20].

Gene context of Lopac-U-101


Analytical, diagnostic and therapeutic context of Lopac-U-101


  1. Regulation of vascular smooth muscle growth by alpha 1-adrenoreceptor subtypes in vitro and in situ. Chen, L., Xin, X., Eckhart, A.D., Yang, N., Faber, J.E. J. Biol. Chem. (1995) [Pubmed]
  2. Studies of alpha-adrenoceptor antagonists on sympathetic mydriasis in rabbits. Yu, Y., Koss, M.C. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics. (2003) [Pubmed]
  3. Differential cardiovascular effects of 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), flesinoxan, 5-methyl-urapidil and MDL 75,608A in conscious spontaneously hypertensive rats. Buisson-Defferier, S., Hibert, M., van den Buuse, M. Fundamental & clinical pharmacology. (1993) [Pubmed]
  4. Cross talk between angiotensin AT1 and alpha 1-adrenergic receptors: angiotensin II downregulates alpha 1a-adrenergic receptor subtype mRNA and density in neonatal rat cardiac myocytes. Li, H.T., Long, C.S., Gray, M.O., Rokosh, D.G., Honbo, N.Y., Karliner, J.S. Circ. Res. (1997) [Pubmed]
  5. The alpha 1A-adrenergic receptor subtype mediates biochemical, molecular, and morphologic features of cultured myocardial cell hypertrophy. Knowlton, K.U., Michel, M.C., Itani, M., Shubeita, H.E., Ishihara, K., Brown, J.H., Chien, K.R. J. Biol. Chem. (1993) [Pubmed]
  6. Use of antisense oligonucleotides to verify the role of the alpha(1A)-adrenergic receptor in the contractility of the rat uterus post partum. Ducza, E., Gáspár, R., Márki, A., Gyula, P., Bottka, S., Falkay, G. Mol. Pharmacol. (2001) [Pubmed]
  7. Renal alpha 1-adrenergic receptor subtypes: MDCK-D1 cells, but not rat cortical membranes possess a single population of receptors. Klijn, K., Slivka, S.R., Bell, K., Insel, P.A. Mol. Pharmacol. (1991) [Pubmed]
  8. Interaction of subtype-selective antagonists with alpha 1-adrenergic receptor-mediated second messenger responses in rat brain. Minneman, K.P., Atkinson, B. Mol. Pharmacol. (1991) [Pubmed]
  9. The alpha(1B)-adrenergic receptor decreases the inotropic response in the mouse Langendorff heart model. Ross, S.A., Rorabaugh, B.R., Chalothorn, D., Yun, J., Gonzalez-Cabrera, P.J., McCune, D.F., Piascik, M.T., Perez, D.M. Cardiovasc. Res. (2003) [Pubmed]
  10. The role of serotonin-1A receptor activation and alpha-1 adrenoceptor blockade in the hypotensive effect of 5-methyl-urapidil. Mandal, A.K., Kellar, K.J., Gillis, R.A. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  11. Beta-adrenoceptor-mediated inhibition of alpha 1-adrenoceptor-mediated and field stimulation-induced contractile responses in the prostate of the guinea pig. Haynes, J.M., Hill, S.J. Br. J. Pharmacol. (1997) [Pubmed]
  12. Characterization of alpha 1-adrenoceptor subtypes in tension response of human prostate to electrical field stimulation. Guh, J.H., Chueh, S.C., Ko, F.N., Teng, C.M. Br. J. Pharmacol. (1995) [Pubmed]
  13. Characterization of alpha1-adrenoceptor subtypes mediating contractions to phenylephrine in rat thoracic aorta, mesenteric artery and pulmonary artery. Hussain, M.B., Marshall, I. Br. J. Pharmacol. (1997) [Pubmed]
  14. Subclassification of alpha 1-adrenoceptor recognition sites by urapidil derivatives and other selective antagonists. Hanft, G., Gross, G. Br. J. Pharmacol. (1989) [Pubmed]
  15. Submandibular gland acinar cells express multiple alpha1-adrenoceptor subtypes. Bockman, C.S., Bruchas, M.R., Zeng, W., O'Connell, K.A., Abel, P.W., Scofield, M.A., Dowd, F.J. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  16. Two pharmacologically distinct alpha 1-adrenoceptor subtypes in the contraction of rabbit aorta: each subtype couples with a different Ca2+ signalling mechanism and plays a different physiological role. Suzuki, E., Tsujimoto, G., Tamura, K., Hashimoto, K. Mol. Pharmacol. (1990) [Pubmed]
  17. Pharmacological characterization of alpha 1-adrenoceptor subtypes in rat heart: a binding study. Noguchi, H., Muraoka, R., Kigoshi, S., Muramatsu, I. Br. J. Pharmacol. (1995) [Pubmed]
  18. Alpha1-adrenoceptor subtypes in rat epididymis and the effects of sexual maturation. Queiróz, D.B., Mendes, F.R., Porto, C.S., Avellar, M.C. Biol. Reprod. (2002) [Pubmed]
  19. (-)-Discretamine, a selective alpha 1D-adrenoceptor antagonist, isolated from Fissistigma glaucescens. Ko, F.N., Guh, J.H., Yu, S.M., Hou, Y.S., Wu, Y.C., Teng, C.M. Br. J. Pharmacol. (1994) [Pubmed]
  20. Differential effects of centrally-active antihypertensives on 5-HT1A receptors in rat dorso-lateral septum, rat hippocampus and guinea-pig hippocampus. Leishman, D.J., Boeijinga, P.H., Galvan, M. Br. J. Pharmacol. (1994) [Pubmed]
  21. Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist. Quaglia, W., Pigini, M., Tayebati, S.K., Piergentili, A., Giannella, M., Leonardi, A., Taddei, C., Melchiorre, C. J. Med. Chem. (1996) [Pubmed]
  22. Functional distribution and role of alpha-1 adrenoceptor subtypes in the mesenteric vasculature of the rat. Kong, J.Q., Taylor, D.A., Fleming, W.W. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  23. Functional studies on alpha 1-adrenoceptor subtypes mediating inotropic effects in rat right ventricle. Michel, M.C., Hanft, G., Gross, G. Br. J. Pharmacol. (1994) [Pubmed]
  24. Urapidil and some analogues with hypotensive properties show high affinities for 5-hydroxytryptamine (5-HT) binding sites of the 5-HT1A subtype and for alpha 1-adrenoceptor binding sites. Gross, G., Hanft, G., Kolassa, N. Naunyn Schmiedebergs Arch. Pharmacol. (1987) [Pubmed]
  25. Role of vascular alpha-1 adrenoceptor subtypes in the pressor response to sympathetic nerve stimulation in the pithed rat. Vargas, H.M., Zhou, L., Gorman, A.J. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  26. alpha-Adrenoceptor antagonists in the treatment of benign prostate hyperplasia. Thiyagarajan, M. Pharmacology (2002) [Pubmed]
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