Evidence that chloroethylclonidine can contract the dog saphenous vein via a protein kinase C-dependent mechanism. 1994

J P Nunes, and A Mota
Institute of Pharmacology and Therapeutics, Faculty of Medicine, Porto, Portugal.

Chloroethylclonidine has recently been shown to produce concentration-dependent contractions in the dog saphenous vein. These contractions are very sensitive to cooling, yohimbine and rauwolscine, and moderately sensitive to prazosin. The effects of compound H-7 (a protein kinase inhibitor) and isradipine (a calcium channel blocker) on the contractions to chloroethylclonidine, UK14304 and phenylephrine were studied in the dog saphenous vein. Compound H-7 (20 mumol/l) produced a very marked (85%) inhibition of chloroethylclonidine-induced contractions, a moderate (48%) inhibition of UK14304-induced contractions and a slight (19%) inhibition of phenylephrine-induced contractions. Isradipine (1 mumol/l) produced a moderate (49%) inhibition of chlorethylclonidine-induced clonidine-induced contractions and a slight (15%) inhibition of phenylephrine-induced contractions. Phorbol 12,13-dibutyrate (1 mumol/l) produced a contraction that reached 61.1 +/- 3.2% of the maximum and was inhibited moderately (46%) by compound H-7. It is suggested that, in the dog saphenous vein, the receptor activated by chloroethylclonidine may be coupled to protein kinase C.

UI MeSH Term Description Entries
D007546 Isoquinolines A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
D008297 Male Males
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D010656 Phenylephrine An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent. (R)-3-Hydroxy-alpha-((methylamino)methyl)benzenemethanol,Metaoxedrin,Metasympatol,Mezaton,Neo-Synephrine,Neosynephrine,Phenylephrine Hydrochloride,Phenylephrine Tannate,Neo Synephrine,Tannate, Phenylephrine
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D011493 Protein Kinase C An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. Calcium Phospholipid-Dependent Protein Kinase,Calcium-Activated Phospholipid-Dependent Kinase,PKC Serine-Threonine Kinase,Phospholipid-Sensitive Calcium-Dependent Protein Kinase,Protein Kinase M,Calcium Activated Phospholipid Dependent Kinase,Calcium Phospholipid Dependent Protein Kinase,PKC Serine Threonine Kinase,Phospholipid Sensitive Calcium Dependent Protein Kinase,Phospholipid-Dependent Kinase, Calcium-Activated,Serine-Threonine Kinase, PKC
D011810 Quinoxalines Quinoxaline
D011942 Receptors, Adrenergic, alpha One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation. Adrenergic alpha-Receptor,Adrenergic alpha-Receptors,Receptors, alpha-Adrenergic,alpha-Adrenergic Receptor,alpha-Adrenergic Receptors,Receptor, Adrenergic, alpha,Adrenergic alpha Receptor,Adrenergic alpha Receptors,Receptor, alpha-Adrenergic,Receptors, alpha Adrenergic,alpha Adrenergic Receptor,alpha Adrenergic Receptors,alpha-Receptor, Adrenergic,alpha-Receptors, Adrenergic
D003000 Clonidine An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION. Catapres,Catapresan,Catapressan,Chlophazolin,Clofelin,Clofenil,Clonidine Dihydrochloride,Clonidine Hydrochloride,Clonidine Monohydrobromide,Clonidine Monohydrochloride,Clopheline,Dixarit,Gemiton,Hemiton,Isoglaucon,Klofelin,Klofenil,M-5041T,ST-155,Dihydrochloride, Clonidine,Hydrochloride, Clonidine,M 5041T,M5041T,Monohydrobromide, Clonidine,Monohydrochloride, Clonidine,ST 155,ST155

Related Publications

J P Nunes, and A Mota
July 1989, The Journal of pharmacology and experimental therapeutics,
J P Nunes, and A Mota
September 1993, Naunyn-Schmiedeberg's archives of pharmacology,
J P Nunes, and A Mota
March 1996, Journal of molecular medicine (Berlin, Germany),
J P Nunes, and A Mota
December 1985, Biochemical and biophysical research communications,
J P Nunes, and A Mota
September 1997, The Journal of pharmacology and experimental therapeutics,
Copied contents to your clipboard!