Literature DB >> 6109637

The blockade of alpha 2-adrenoceptors by the PNMT inhibitaor SK&F 64139.

M Goldstein, M Saito, J Y Lew, J P Hieble, R G Pendleton.   

Abstract

Three tetrahydroisoquinolines were tested for activity on central alpha 2-adrenoceptors by determining their ability to inhibit [3H]clonidine binding to rat cerebral cortical membrane homogenates. The compounds included the PNMT inhibitors SK&F 64139 (7,8-dichloro-1,2,3,4-tetrahydroisoquinoline) and SK&F 29661 (1,2,3,4-tetrahydroisoquinoline 7-sulfonamide) as well as SK&F 72223 (5,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline) a structural analogue inactive as a PNMT inhibitor. SK&F 64139 and SK&F 72223 but not SK&F 29661 inhibited [3H]clonidine binding. Studies in the isolated guinea pig atrium confirmed that SK&F 64139 and SK&F 72223 are alpha 2-adrenoceptor antagonists.

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Year:  1980        PMID： 6109637     DOI： 10.1016/0014-2999(80)90513-0

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  5 in total

1.  Application of the Goldilocks effect to the design of potent and selective inhibitors of phenylethanolamine N-methyltransferase: balancing pKa and steric effects in the optimization of 3-methyl-1,2,3,4-tetrahydroisoquinoline inhibitors by beta-fluorination.

Authors:  Gary L Grunewald; Mitchell R Seim; Jian Lu; Mariam Makboul; Kevin R Criscione
Journal:  J Med Chem       Date:  2006-05-18       Impact factor: 7.446

2.  An insulin-releasing property of imidazoline derivatives is not limited to compounds that block alpha-adrenoceptors.

Authors:  A Schulz; A Hasselblatt
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-09       Impact factor: 3.000

3.  Studies on the long term effects of SK&F 29661 upon adrenal catecholamines.

Authors:  R G Pendleton; G Gessner; J Sawyer; L Hillegass; D A Miller
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1982-04       Impact factor: 3.000

4.  The influence of SK & F 64139, a phenylethanolamine-N-methyltransferase inhibitor, on centrally mediated cardiovascular effects of alpha-methyldopa and clonidine.

Authors:  M Gerold; G Haeusler
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1982-12       Impact factor: 3.000

5.  The Adrenal Medulla Modulates Mechanical Allodynia in a Rat Model of Neuropathic Pain.

Authors:  Marina Arribas-Blázquez; Luis Alcides Olivos-Oré; María Victoria Barahona; Aneta Wojnicz; Ricardo De Pascual; Mercedes Sánchez de la Muela; Antonio G García; Antonio R Artalejo
Journal:  Int J Mol Sci       Date:  2020-11-06       Impact factor: 5.923
  5 in total

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