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Chemical Compound Review:

Tocris-1054 3-(3-dimethylaminopropyl)-4- hydroxy-N-(4...

Synonyms: CHEMBL119264, SureCN3366363, CHEBI:295260, BPBio1_000002, GR-55562, ...

Maassen VanDenBrink, A. et al., Yamada, J. et al., Banes, A.K. et al., MacLean, M.R. et al., Walsh, D.M. et al.

Yamada, Sugimoto, Hirose, Kajiwara, Banes, Watts,

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High impact information on GR55562

In the CH rats the estimated pKb values for GR55562 were 6.5, 7.8 and 7.0 in the pulmonary resistance arteries, first branch and main pulmonary artery, respectively [1].
The suppressive effects of leptin on milk intake were antagonized by the 5-HT(2B/2C) receptor antagonist SB206553, while the 5-HT(1B) receptor antagonist GR55562 and the 5-HT(2A) receptor antagonist ketanserin did not affect it [2].
In contrast, GR55562 and methiothepin behaved as competitive 5-HT1D receptor antagonists and were devoid of any agonist activity [3].
The 5-HT(1B) receptor antagonist GR55562 (100 nmol/L) inhibited both the 5-HT- (4-fold rightward shift) and CP93129-induced (11-fold rightward shift) contractions in mesenteric arteries from hypertensive DOCA-salt rats [4].
Human isolated coronary artery contraction to sumatriptan characterised by the selective 5-HT1B/1D receptor antagonist GR55562 [5].

Associations of GR55562 with other chemical compounds

Using the agonists sumatriptan and 5-carboxamidotryptamine and the selective 5-HT1B/1D receptor antagonist GR55562, we have investigated the involvement of 5-HT1B/1D receptors in the contraction of the human isolated coronary artery [5].

Gene context of GR55562

The pA2 of GR55562 (7.40+/-0.16) was in accord with its reported affinity at the human 5-HT1B receptor [5].

References

5-Hydroxytryptamine receptors mediating vasoconstriction in pulmonary arteries from control and pulmonary hypertensive rats. MacLean, M.R., Sweeney, G., Baird, M., McCulloch, K.M., Houslay, M., Morecroft, I. Br. J. Pharmacol. (1996) [Pubmed]
Role of serotonergic mechanisms in leptin-induced suppression of milk intake in mice. Yamada, J., Sugimoto, Y., Hirose, H., Kajiwara, Y. Neurosci. Lett. (2003) [Pubmed]
The activity of 5-HT1D receptor ligands at cloned human 5-HT1D alpha and 5-HT1D beta receptors. Walsh, D.M., Beattie, D.T., Connor, H.E. Eur. J. Pharmacol. (1995) [Pubmed]
Enhanced contraction to 5-hydroxytryptamine is not due to "unmasking" of 5-hydroxytryptamine(1b) receptors in the mesenteric artery of the deoxycorticosterone acetate-salt rat. Banes, A.K., Watts, S.W. Hypertension (2001) [Pubmed]
Human isolated coronary artery contraction to sumatriptan characterised by the selective 5-HT1B/1D receptor antagonist GR55562. Maassen VanDenBrink, A., Reekers, M., Bax, W.A., Saxena, P.R. Pharmacol. Toxicol. (2000) [Pubmed]

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