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Chemical Compound Review

Lopac-B-134     8-[2-[4-(2- methoxyphenyl)piperazin-1...

Synonyms: Tocris-1006, CHEMBL13647, Bmy-7378, AG-K-27251, SureCN6017145, ...
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Disease relevance of BMY7378


Psychiatry related information on BMY7378


High impact information on BMY7378

  • There were no effects of the 5-HT1a antagonist, BMY 7378, or the 5-HT3 antagonist, MDL 72222.(ABSTRACT TRUNCATED AT 250 WORDS)[7]
  • The negative geotaxis was impaired after all 5-HT1A receptor ligands, except BMY 7378 and (+/-)-WAY 100,135 [8].
  • In alpha1D fibroblasts, BMY 7378 inhibited growth and protected alpha1D-ARs from CEC alkylation while having little blocking or protecting effect on the growth induced by stimulation of fibroblasts that express alpha1A- or alpha1B-ARs [9].
  • No significant changes in pHi were observed with cells treated with alpha 1D-AR antisense ODNs or the alpha 1D-AR antagonist BMY 7378 compared with untreated cells [10].
  • In contrast, whereas the maximal inhibition of cortical 5-HTP accumulation by BMY 7378 (55%) was similar to that obtained with the agonists, maximal response in the hippocampus was much smaller (32%) [11].

Chemical compound and disease context of BMY7378


Biological context of BMY7378

  • [3H]-silodosin binding sites also showed high affinity for silodosin and tamsulosin but low sensitivity to BMY 7378 (8-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-8-azaspiro(4.5)decane-7,9-dione) (Research Biochemicals International) in intact segments and in membrane preparations [13].
  • 6. Stimulation of PI hydrolysis induced by phenylephrine was not affected by BMY 7378 up to 10 nM but it was reduced significantly by BMY 7378 at higher concentrations (100 nM to 1 microM) [14].
  • Further, BMY 7378 is able to phase advance circadian rhythms by approximately 1 h at night even without light exposure [15].
  • Although BMY-7378 and NAN-190 both displayed high affinity for the 5-HT1A receptor (IC50 values of 0.8 and 7.5 nM, respectively), their effects, when administered alone, as well as in combination with 8-OH-DPAT, were distinct [16].
  • The putative 5-HT1A receptor antagonist BMY 7378 (3-100 i.v.) caused reductions in blood pressure, heart rate and efferent renal nerve activity in anaesthetised cats [3].

Anatomical context of BMY7378

  • In the thoracic aorta, pA(2) values in WT mice for KMD-3213 and BMY7378 were 8.25 and 8.46, respectively, and in alpha(1B)-KO mice they were 8.49 and 9.13, respectively [17].
  • 4. BMY 7378 was approximately 100 fold more potent as an antagonist of phenylephrine on aortic strips (pA2 9.0 +/- 0.13) than on vas deferens (pKB 7.17 +/- 0.08) and spleen (pKB 7.16 +/- 0.21); it was ineffective on the prostate [18].
  • Pharmacological evidence for alpha(1D)-adrenoceptors in the rabbit ventricular myocardium: analysis with BMY 7378 [14].
  • These pharmacological findings were in fairly good agreement with findings from comparison of CRCs, with the exception of the mesenteric arteries of WT and alpha(1B)-KO mice, which showed low affinities to BMY7378 [17].
  • BMY 7378 bound to membranes expressing the cloned rat alpha-1D AR with a > 100-fold higher affinity (K1 = 2 nM) than binding to either the cloned rat alpha-1A AR (Ki = 800 nM) or the hamster alpha-1B AR (Ki = 600 nM) [19].

Associations of BMY7378 with other chemical compounds

  • These characteristics clearly distinguish 14 from previously-reported ligands such as the postsynaptic 5-HT1A antagonist BMY 7378 and the weak partial agonist NAN 190 which, in contrast to the compounds of this series, belong to the well-exemplified class of imido derivatives of (o-methoxyphenyl)piperazines [20].
  • 4. Prazosin, 5-methylurapidil and BMY7378 acted competitively in alpha(1B)-KO carotid arteries with pA(2) of 10.3, 7.6 and 9.6, respectively [21].
  • 3. BMY 7378 (8 mg kg-1, s.c.) inhibited another effect of activation of postsynaptic 5-HT1A receptors, i.e., the induction of components of the 5-HT syndrome by 8-OH-DPAT (0.5, 1.0 mg kg-1, s.c.) which suggests that BMY 7378 has antagonistic as well as agonistic effects at these sites [2].
  • Conversely, the increase in perfusion pressure induced by micromolar concentrations of phenylephrine was blocked by 1 nM (+)-niguldipine, but was unaffected by BMY 7378 [22].
  • In SHR aorta BMY 7378 protected alpha(1D)-adrenoceptors and in caudal arteries 5-methylurapidil protected alpha(1A)-adrenoceptors from chloroethylclonidine alkylation, allowing noradrenaline to elicit contraction [23].

Gene context of BMY7378


Analytical, diagnostic and therapeutic context of BMY7378

  • The depressant effects of microiontophoretically-applied tandospirone and 5-HT, on the firing activity of CA3 pyramidal neurones in the hippocampus were blocked by the intravenous injection of the 5-HT1A receptor antagonist, BMY-7378 [29].
  • In contrast to its apparent 5-HT1A antagonist properties in the behavioural experiments, BMY 7378 caused a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis [30].
  • OBJECTIVE: To evaluate the effect of the nonselective purinergic antagonist suramin and the alpha1-adrenergic antagonists, terazosin and BMY 7378, given intravenously or infused directly into the bladder during cystometry in conscious rats with bladder outlet obstruction induced by urethral ligation [31].


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  3. BMY 7378 is an agonist at 5-HT1A receptors mediating hypotension and renal sympatho-inhibition in anaesthetised cats. Stubbs, C.M., Connor, H.E., Feniuk, W. Eur. J. Pharmacol. (1991) [Pubmed]
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  10. Proximal nephron Na+/H+ exchange is regulated by alpha 1A- and alpha 1B-adrenergic receptor subtypes. Liu, F., Nesbitt, T., Drezner, M.K., Friedman, P.A., Gesek, F.A. Mol. Pharmacol. (1997) [Pubmed]
  11. Receptor reserve for 5-hydroxytryptamine1A-mediated inhibition of serotonin synthesis: possible relationship to anxiolytic properties of 5-hydroxytryptamine1A agonists. Meller, E., Goldstein, M., Bohmaker, K. Mol. Pharmacol. (1990) [Pubmed]
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  13. Identification of alpha-1L and alpha-1A adrenoceptors in human prostate by tissue segment binding. Morishima, S., Tanaka, T., Yamamoto, H., Suzuki, F., Akino, H., Yokoyama, O., Muramatsu, I. J. Urol. (2007) [Pubmed]
  14. Pharmacological evidence for alpha(1D)-adrenoceptors in the rabbit ventricular myocardium: analysis with BMY 7378. Yang, H.T., Endoh, M. Br. J. Pharmacol. (1997) [Pubmed]
  15. Serotonergic serotonin (1A) mixed agonists/antagonists elicit large-magnitude phase shifts in hamster circadian wheel-running rhythms. Gannon, R.L. Neuroscience (2003) [Pubmed]
  16. Antagonism studies with BMY-7378 and NAN-190: effects on 8-hydroxy-2-(di-n-propylamino)tetralin-induced increases in punished responding of pigeons. Ahlers, S.T., Weissman, B.A., Barrett, J.E. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  17. Correlation between vasoconstrictor roles and mRNA expression of alpha1-adrenoceptor subtypes in blood vessels of genetically engineered mice. Hosoda, C., Tanoue, A., Shibano, M., Tanaka, Y., Hiroyama, M., Koshimizu, T.A., Cotecchia, S., Kitamura, T., Tsujimoto, G., Koike, K. Br. J. Pharmacol. (2005) [Pubmed]
  18. Characterization of alpha 1 D-adrenoceptor subtype in rat myocardium, aorta and other tissues. Deng, X.F., Chemtob, S., Varma, D.R. Br. J. Pharmacol. (1996) [Pubmed]
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  20. Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines. Peglion, J.L., Canton, H., Bervoets, K., Audinot, V., Brocco, M., Gobert, A., Le Marouille-Girardon, S., Millan, M.J. J. Med. Chem. (1995) [Pubmed]
  21. Insights into the functional roles of alpha(1)-adrenoceptor subtypes in mouse carotid arteries using knockout mice. Deighan, C., Methven, L., Naghadeh, M.M., Wokoma, A., Macmillan, J., Daly, C.J., Tanoue, A., Tsujimoto, G., McGrath, J.C. Br. J. Pharmacol. (2005) [Pubmed]
  22. alpha(1D)-adrenoceptors cause endothelium-dependent vasodilatation in the rat mesenteric vascular bed. Filippi, S., Parenti, A., Donnini, S., Granger, H.J., Fazzini, A., Ledda, F. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  23. Differential response to chloroethylclonidine in blood vessels of normotensive and spontaneously hypertensive rats: role of alpha 1D- and alpha 1A-adrenoceptors in contraction. Ibarra, M., Pardo, J.P., Lopez-Guerrero, J.J., Villalobos-Molina, R. Br. J. Pharmacol. (2000) [Pubmed]
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  27. Serotonin inhibits luteinizing hormone release via 5-HT1A receptors in the zona incerta of ovariectomised, anaesthetised rats primed with steroids. Siddiqui, A., Kotecha, K., Salicioni, A.M., Kalia, V., Murray, J.F., Wilson, C.A. Neuroendocrinology (2000) [Pubmed]
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  30. Further investigation of the in vivo pharmacological properties of the putative 5-HT1A antagonist, BMY 7378. Sharp, T., Backus, L.I., Hjorth, S., Bramwell, S.R., Grahame-Smith, D.G. Eur. J. Pharmacol. (1990) [Pubmed]
  31. Effects of intravenous and infravesical administration of suramin, terazosin and BMY 7378 on bladder instability in conscious rats with bladder outlet obstruction. Velasco, C., Guarneri, L., Leonardi, A., Testa, R. BJU international. (2003) [Pubmed]
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