Actions of tetrahydropapaveroline on the cardiovascular system and skeletal muscles of the anaesthetized cat and on guinea-pig soleus muscle in vitro. 1978

M W Nott, and G A Head

1. Tetrahydropapaveroline (THP) and isoprenaline have been compared for effects on heart rate, diastolic blood pressure and contractions of soleus and tibialis muscles in chloralose-anaesthetized cats and on in vitro guinea-pig soleus muscles. 2. All effects of THP were similar to those of isoprenaline. Maximal responses were the same and responses to both drugs were antagonized by propranolol. 3. THP produced an increase in heart rate, a fall in diastolic blood pressure and a decrease in the tension and degree of fusion of incomplete tetanic contractions of the soleus, being, respectively, 12.9, 14.7 and 19.6 times less potent than isoprenaline. The similarity in potency ratios suggests that THP is a non-selective beta-adrenoceptor agonist. 4. Effects on the guinea-pig soleus in vitro were similar to those in the cat soleus. 5. In the cat, THP enhanced the tension and duration of tibialis twitches, but the tibialis was about ten times less sensitive than the soleus to the effects of THP. 6. THP deepened neuromuscular blockade in partially curarized cat soleus and tibialis preparations. Doses required were ten times greater than for direct depressant effects on the soleus. 7. Agents which depress the tension and fusion of incomplete tetanic contractions of the cat soleus via beta-adrenoceptor stimulation cause tremor in man by peripheral effects on slow muscle fibres. THP is likely to exert such actions. This may explain why levodopa (a precursor of THP) sometimes precipitates a tremor crisis in Parkinsoniam patients, and why Parkinsonian tremor is relatively refractory to levodopa therapy. In such patients combination therapy with levodopa and a peripheral dopa decarboxylase inhibi;or (to reduce levels of THP) or a beta-adrenoceptor antagonist (to block the effects of THP on slow muscle fibres) could be advantageous.

UI MeSH Term Description Entries
D007545 Isoproterenol Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant. Isoprenaline,Isopropylarterenol,4-(1-Hydroxy-2-((1-methylethyl)amino)ethyl)-1,2-benzenediol,Euspiran,Isadrin,Isadrine,Isopropyl Noradrenaline,Isopropylnoradrenaline,Isopropylnorepinephrine,Isoproterenol Hydrochloride,Isoproterenol Sulfate,Isuprel,Izadrin,Norisodrine,Novodrin,Hydrochloride, Isoproterenol,Noradrenaline, Isopropyl,Sulfate, Isoproterenol
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
D010208 Papaverine An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels. Cerespan,Papaverine Hydrochloride,Pavabid,Pavatym,Hydrochloride, Papaverine
D001794 Blood Pressure PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS. Systolic Pressure,Diastolic Pressure,Pulse Pressure,Pressure, Blood,Pressure, Diastolic,Pressure, Pulse,Pressure, Systolic,Pressures, Systolic
D002415 Cats The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801) Felis catus,Felis domesticus,Domestic Cats,Felis domestica,Felis sylvestris catus,Cat,Cat, Domestic,Cats, Domestic,Domestic Cat
D002698 Chloralose A derivative of CHLORAL HYDRATE that was used as a sedative but has been replaced by safer and more effective drugs. Its most common use is as a general anesthetic in animal experiments. Anhydroglucochloral,Glucochloral,Glucochloralose,alpha-Chloralose,beta-Chloralose,alpha Chloralose,beta Chloralose
D005260 Female Females
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006339 Heart Rate The number of times the HEART VENTRICLES contract per unit of time, usually per minute. Cardiac Rate,Chronotropism, Cardiac,Heart Rate Control,Heartbeat,Pulse Rate,Cardiac Chronotropy,Cardiac Chronotropism,Cardiac Rates,Chronotropy, Cardiac,Control, Heart Rate,Heart Rates,Heartbeats,Pulse Rates,Rate Control, Heart,Rate, Cardiac,Rate, Heart,Rate, Pulse

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