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Chemical Compound Review:

Lopac-S-174 2-diethylaminoethyl 4-amino-5-chloro-2...

Synonyms: CHEMBL287045, AG-J-54777, SureCN1038983, ACMC-20cut4, CHEBI:145979, ...

Eglen, R.M. et al., Espejo, E.F. et al., Kuemmerle, J.F. et al., François, A. et al., Tuladhar, B.R. et al., et al.

Kellum, Albuquerque, Stoner, Harris,

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Disease relevance of SDZ 205-557

In the anaesthetized, vagotomized micropig, SDZ 205,557 produced only a transient blockade of 5-HT4-mediated tachycardia [1].

High impact information on SDZ 205-557

RESULTS: 5-HT binding was completely inhibited by 5-HT and partially by 5-HT2A (ketanserin), 5-HT4 (SDZ-205,557), and 5-HT1p (N-acetyl-5-hydroxytryptophyl-5-hydroxytryptophan amide; 5-HTP-DP) receptor antagonists [2].
In cells with only 5-HT4/5-HT1p receptors, 5-HT caused only relaxation and residual binding was inhibited by SDZ-205,557 and 5-HTP-DP [2].
8c is an antagonist equipotent to the 5-HT4 receptor antagonist SDZ 205-557 (1) [3].
Tissue responses to exogenously added 5-HT (nonneural pathway) and electrical field stimulation (EFS; neural pathway) were performed, and 5-HT receptor subtypes implicated in both responses were determined using three different 5-HT receptor antagonists: methysergide (5-HT(2/1C)), granisetron (5-HT(3)), and SDZ-205,557 (5-HT(4)) [4].
Intra-NAc shell microinjections of either RS 67333 (1 or 3 microgram/0.2 microliter/side) or SDZ 205,557 (1-5 microgram/0.2 microliter/side) did not alter spontaneous activity observed after a systemic saline injection but did significantly attenuate the hyperactivity induced by systemic cocaine injection (10 mg/kg) [5].

Biological context of SDZ 205-557

3. In functional studies of 5-HT3 receptors, SDZ 205,557 exhibited an affinity of 6.2 in guinea-pig ileum compared with 6.9 at binding sites labelled by [3H]-quipazine in NG108-15 cells [1].

Anatomical context of SDZ 205-557

2. In guinea-pig hippocampus and in the presence of 0.4 microM 5-carboxamidotryptamine, 5-HT4-mediated stimulation of adenylyl cyclase was competitively antagonized by SDZ 205,557, with a pA2 value of 7.5, and a Schild slope of 0.81 [1].
5-HT4 receptors, present in piglet atria and sensitive to SDZ 205-557, are absent in papillary muscle [6].
4. Serotonin neither contracted nor relaxed the canine esophagus and relaxed the rat esophagus via 5-HT4 receptor activation as determined by antagonism with ICS 205-930 (-log KB = 6.4), metoclopramide (-log KB = 6.7) and its ester congener SDZ 205-557 (-log KB = 7.9) [7].

Associations of SDZ 205-557 with other chemical compounds

[3a-Tropanyl]-1H-indole-3-carboxylic acid ester (tropisetron) and 2-methoxy-4-amino-5-chloro-benzoic acid 2-(diethylamino)ethyl ester (SDZ 205-557), two other 5-HT4 receptor antagonists, mimicked the effects of DAU 6285 [8].
GR 113808, SDZ 205-557 and DAU 6285 all functioned as competitive antagonists at these 5-HT4 receptors [9].
In rat carbachol-contracted oesophagus, 5-HT4-receptor mediated relaxations were surmountably antagonized by SDZ 205,557 with a similar pA2 value (7.3) [1].
9 It is concluded that the relaxant response to 5-HT in the terminal region of the ileum is mediated directly at the smooth muscle; a ranked indole agonist potency and selective antagonism by 5-HT4 receptor antagonists tropisetron, SDZ 205-557 and GR 113808 indicate a 5-HT4 receptor involvement in the relaxation response [10].
In this paper, SDZ 205-557 (2-methoxy-4-amino-5-chloro-benzoic acid 2-(diethylamino) ethyl ester) is characterized as the first potent, selective and surmountable antagonist at 5-HT4 receptors in the isolated guinea pig ileum [11].

Gene context of SDZ 205-557

The objective of this study was to establish the activity profile of SDZ 205-557, a 5-HT4 antagonist, on cutaneous (hotplate) and visceral (writhing) models of pain, after peripheral administration [12].
It was also inhibited by the 5-HT(3,4) receptor antagonist tropisetron (10 microM) and the 5-HT(4,3) receptor antagonist SDZ-205-557 (10 microM) but not by preferential antagonists of 5-HT(1P), 5-HT(2A), or 5-HT3 receptors [13].

Analytical, diagnostic and therapeutic context of SDZ 205-557

SDZ 205-557 also induced hypoalgesia in the writhing test over the entire dose range tested, and visceral hypoalgesia turned out to be analgesia after 1:1 combination [12].

References

The action of SDZ 205,557 at 5-hydroxytryptamine (5-HT3 and 5-HT4) receptors. Eglen, R.M., Alvarez, R., Johnson, L.G., Leung, E., Wong, E.H. Br. J. Pharmacol. (1993) [Pubmed]
Coexpression of 5-HT2A and 5-HT4 receptors coupled to distinct signaling pathways in human intestinal muscle cells. Kuemmerle, J.F., Murthy, K.S., Grider, J.R., Martin, D.C., Makhlouf, G.M. Gastroenterology (1995) [Pubmed]
Arylcarbamate derivatives of 1-piperidineethanol as potent ligands for 5-HT4 receptors. Soulier, J.L., Yang, D., Brémont, B., Croci, T., Guzzi, U., Langlois, M. J. Med. Chem. (1997) [Pubmed]
Changes in 5-HT-mediated pathways in radiation-induced attenuation and recovery of ion transport in rat colon. François, A., Ksas, B., Gourmelon, P., Griffiths, N.M. Am. J. Physiol. Gastrointest. Liver Physiol. (2000) [Pubmed]
Antagonism of 5-hydroxytryptamine(4) receptors attenuates hyperactivity induced by cocaine: putative role for 5-hydroxytryptamine(4) receptors in the nucleus accumbens shell. McMahon, L.R., Cunningham, K.A. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
5-HT4 receptors, present in piglet atria and sensitive to SDZ 205-557, are absent in papillary muscle. Lorrain, J., Grosset, A., O'Connor, S.E. Eur. J. Pharmacol. (1992) [Pubmed]
5-HT4 receptors in rat but not guinea pig, rabbit or dog esophageal smooth muscle. Cohen, M.L., Susemichel, A.D., Bloomquist, W., Robertson, D.W. Gen. Pharmacol. (1994) [Pubmed]
Pharmacological analyses of endo-6-methoxy-8-methyl-8-azabicyclo[3.2.1]oct-3-yl-2,3-dihydro-2-oxo-1 H- benzimidazole-1-carboxylate hydrochloride (DAU 6285) at the 5-hydroxytryptamine4 receptor in the tunica muscularis mucosae of rat esophagus and ileum of guinea pig: role of endogenous 5-hydroxytryptamine. Waikar, M.V., Hegde, S.S., Ford, A.P., Clarke, D.E. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
Antagonists of 5-HT4 receptor-mediated responses in adult hippocampal neurons. Torres, G.E., Holt, I.L., Andrade, R. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
Pharmacological characterization of the 5-hydroxytryptamine receptor mediating relaxation in the rat isolated ileum. Tuladhar, B.R., Costall, B., Naylor, R.J. Br. J. Pharmacol. (1996) [Pubmed]
SDZ 205-557, a selective, surmountable antagonist for 5-HT4 receptors in the isolated guinea pig ileum. Buchheit, K.H., Gamse, R., Pfannkuche, H.J. Naunyn Schmiedebergs Arch. Pharmacol. (1992) [Pubmed]
Antagonism of peripheral 5-HT4 receptors reduces visceral and cutaneous pain in mice, and induces visceral analgesia after simultaneous inactivation of 5-HT3 receptors. Espejo, E.F., Gil, E. Brain Res. (1998) [Pubmed]
Stroking human jejunal mucosa induces 5-HT release and Cl- secretion via afferent neurons and 5-HT4 receptors. Kellum, J.M., Albuquerque, F.C., Stoner, M.C., Harris, R.P. Am. J. Physiol. (1999) [Pubmed]

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