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Chemical Compound Review:

CHEMBL26717 1,2,3,4- tetrahydroisoquinoline-7- sulfonamide

Synonyms: AG-F-04658, SureCN1487047, CHEBI:45649, SKF-29661, KST-1B3111, ...

Pendleton, R.G. et al., Pendleton, R.G. et al., Blank, B. et al., Grunewald, G.L. et al., Black, J. et al.

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High impact information on 1,2,3,4-TETRAHYDRO-ISOQUINOLINE-7-SULFONIC ACID AMIDE

In the rats given SK&F 29661, practically no acute blood pressure changes were in the adrenal glands [1].
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor [2].
1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides (1-14) related to 1,2,3,4-tetrahydroisoquinoline-7-sulfonamide (21,SK&F 29661) were prepared and studied for their ability to inhibit phenylethanolamine N-methyltransferase (PNMT) in vitro [3].
SK&F 29661 did not, however, reduce rat brain stem PNMT activity after systemic administration; subsequent radioautographic studies indicated that the compound did not enter the central nervous system, presumably because of its high polarity [4].

Associations of 1,2,3,4-TETRAHYDRO-ISOQUINOLINE-7-SULFONIC ACID AMIDE with other chemical compounds

This effect of the drug was accompanied by a prolonged hypotensive period and was not seen with SK&F 29661, a selective inhibitor of peripheral (adrenal) PNMT or with SK&F 72223, a structural analog of SK&F 64139 which has no effect on PNMT [5].

References

Blood pressure response to central and/or peripheral inhibition of phenylethanolamine N-methyltransferase in normotensive and hypertensive rats. Black, J., Waeber, B., Bresnahan, M.R., Gavras, I., Gavras, H. Circ. Res. (1981) [Pubmed]
Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. Grunewald, G.L., Dahanukar, V.H., Caldwell, T.M., Criscione, K.R. J. Med. Chem. (1997) [Pubmed]
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides. Blank, B., Krog, A.J., Weiner, G., Pendleton, R.G. J. Med. Chem. (1980) [Pubmed]
Studies on SK&F 29661, an organ-specific inhibitor of phenylethanolamine N-methyltransferase. Pendleton, R.G., Gessner, G., Weiner, G., Jenkins, B., Sawyer, J., Bondinell, W., Intoccia, A. J. Pharmacol. Exp. Ther. (1979) [Pubmed]
The effects of PNMT inhibitors upon cardiovascular changes induced by hemorrhage in the rat. Pendleton, R.G., McCafferty, J.P., Roesler, J.M. Eur. J. Pharmacol. (1980) [Pubmed]

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