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Chemical Compound Review

CHEMBL24999     (7R,8R)-7-benzhydryl-N-[(2...

Synonyms: CHEBI:133778, AC1L31BT, L-703606, L703606, L 703606, ...
 
 
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High impact information on L 703606

  • (cis)-2-(Diphenylmethyl)-N-[(2-iodophenyl)-methyl]-1- azabicyclo[2.2.2]octan-3-amine (L-703606) inhibits binding of 125I-Tyr8-substance P to the human NK1 receptor with an IC50 of 2 nM [1].
  • Pituitaries of both sexes preincubated with medium-alone, GnRH, GnRH plus L-703606, and GnRH plus SP plus L-703606 increased steroid secretion during prereproduction, noncourtship, courtship, and recovery; the increase induced by the pituitaries incubated with medium-alone was lower during prereproduction, noncourtship, and recovery [2].
  • Preincubation with SP or the NK1 receptor antagonist L-703606 prevented GPSP marking [3].
  • On coronary strips in vitro, which had been precontracted with U46619, GPSP induced relaxations similar to those produced by equimolar concentrations of SP, both relaxations being inhibited by L-703606 [3].
  • The positive inotropic effect of lysophosphatidic acid in vivo was not affected by the blockers of angiotensin II, endothelin-1, or adrenergic receptors, but this action was abolished by pretreatment with neurokinin type 1 receptor antagonist (L703606) as well as Ca2+-channel antagonist (verapamil) [4].
 

Gene context of L 703606

  • During prereproduction, reproduction (noncourtship and courtship), refractory, recovery and aestivation, male and female pituitaries were incubated with medium-alone, GnRH, SP, GnRH receptor antagonist (antide), and SP receptor antagonist (L-703606) [2].

References

  1. Characterization of the binding of a potent, selective, radioiodinated antagonist to the human neurokinin-1 receptor. Cascieri, M.A., Ber, E., Fong, T.M., Sadowski, S., Bansal, A., Swain, C., Seward, E., Frances, B., Burns, D., Strader, C.D. Mol. Pharmacol. (1992) [Pubmed]
  2. Substance P downregulates basal and gonadotropin-releasing hormone-induced gonadotropin in vitro secretion by pituitary gland of crested newt, Triturus carnifex. Gobbetti, A., Petrelli, C., Zerani, M. J. Neuroendocrinol. (2000) [Pubmed]
  3. Binding of gold-protein ligand complexes to neurokinin receptors. visualization with the electron microscope on pig coronary artery and rat portal vein. Cathieni, M.M., Taban, C.H., Sors, P., Mastrangelo, D. J. Vasc. Res. (1999) [Pubmed]
  4. Mechanism of the positive inotropic effect of lysophosphatidic acid in rat heart. Xu, Y.J., Rathi, S.S., Zhang, M., Bhugra, P., Dhalla, N.S. J. Cardiovasc. Pharmacol. Ther. (2002) [Pubmed]
 
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