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Biomedical subjects

C Raper

Publications and source records attributed to C Raper.

At least 55 records · Page 3Linked to original sources
PubMed1972

Use of cumulative dose-response curves in potency comparisons of sympathomimetic amines on the cat soleus muscle.

The ability of beta-adrenoceptor agonists to reduce the fusion of incomplete tetanic contractions of the soleus muscle of the cat has been used previously as a model to assess the potential tremor producing effect of sympathomimetic bronchodilators. The ability of (-)-isoprenaline, (-)-adrenaline, (+/-)-soterenol and (+/-)-quinterenol to depress incomplete tetanic contractions of the soleus has now been assessed using cumulative administration of the amines. The method quickly produced accurate and reproducible dose-response curves. It is particularly useful for evaluating the potency of long-acting compounds.

Animals↗
PubMed1972

Pharmacological actions of a new -adrenoceptor agonist, MJ-9184-1, in anaesthetized cats.

1. The effects of (-)-isoprenaline and the new beta-adrenoceptor agonist, MJ-9184-1, on the lungs, on the cardiovascular system, and on slow contracting skeletal muscle have been compared in cats under chloralose anaesthesia.2. Both amines reduced the increases in airways resistance produced by 5-HT, depressed incomplete tetanic contractions of the soleus muscle, lowered the blood pressure and produced an increase in heart rate. In comparison with (-)-isoprenaline, MJ-9184-1 had a long duration of action.3. The effects of MJ-9184-1 and (-)-isoprenaline were antagonized by the beta-adrenoceptor antagonist, propranolol.4. MJ-9184-1 was approximately half as potent as (-)-isoprenaline in its effects on pulmonary resistance and soleus muscle contractility, and one seventh as potent in producing chronotropic effects in the heart.5. These results suggest that MJ-9184-1 possesses some specificity as a beta(2) receptor stimulant.

Adrenergic beta-Agonists↗
PubMed1971

Pyrrolizidine alkaloids: actions on muscarinic receptors in the guinea-pig ileum.

1. Eleven pyrrolizidine alkaloids have been tested on the isolated guinea-pig ileum preparation.2. Platyphylline, supinine, heleurine and cynaustraline were more potent in antagonizing responses to acetylcholine and carbachol than responses to histamine. Their anticholinergic activity appeared to involve a competitive mechanism.3. Lasiocarpine, monocrotaline, spectabiline, sarracine, 7-angelylheliotridine, heliotrine and senecionine had similar antagonistic potencies against responses to both acetylcholine and histamine.4. The alkaloids had no appreciable activity as antagonists of acetylcholine in the isolated toad rectus abdominis preparation.5. These results are discussed with respect to interactions of the alkaloids at receptor sites involved in anticholinergic activity at the muscarinic receptor.

Acetylcholine↗
PubMed1970

Prejunctional actions of some beta-adrenoreceptor antagonists in the vas deferens preparation of the guinea-pig.

1. The beta-adrenoceptor antagonists propranolol, pronethalol, MJ 1999 and Ciba 39089-Ba reduced responses to field stimulation of the guinea-pig isolated vas deferens preparation without significantly affecting responses to exogenously added noradrenaline.2. This prejunctional blocking action of the drugs cannot be correlated with their action as beta-adrenoceptor antagonists or non-specific depressants.3. The blockade produced was more pronounced at low (5-20 Hz) than at high (50 Hz) frequencies of stimulation.4. The blockade was slow in onset, and once established was poorly reversed by washing the preparation over a period of 1 to 2 h.5. The blockade produced could be reversed by dexamphetamine and cocaine.6. These experiments suggest that the beta-adrenoceptor antagonists may have some actions which closely resemble those of the adrenergic neurone blocking agent guanethidine.

Adrenergic beta-Antagonists↗
PubMed1970

Mephenesin, methocarbamol, chlordiazepoxide and diazepam: actions on spinal reflexes and ventral root potentials.

1. Dose levels of mephenesin, methocarbamol, chlordiazepoxide and diazepam which abolished polysynaptic reflex contractions had no effect on monosynaptic knee-jerk reflexes in chloralose anaesthetized cats.2. Ventral root potentials were recorded following stimulation of the corresponding dorsal root (L7 or S1), and the areas of the mono- and polysynaptic components were measured by planimetry.3. Dose levels of the drugs which abolished polysynaptic reflex contractions reduced the areas of the polysynaptic component of the ventral root potentials by about 50%. Mephenesin and methocarbamol reduced the area of the monosynaptic component to a similar extent. Chlordiazepoxide was less potent in this respect while diazepam was without effect at this dose level.4. Linear regression lines were calculated for the reduction in the mono- and polysynaptic components of ventral root potentials with increasing doses of each of the four drugs. With methocarbamol and mephenesin the lines were parallel and coincident. With chlordiazepoxide and diazepam they were parallel but not coincident. Large doses of diazepam were required to reduce the area of the monosynaptic component, this drug being the only one of the four tested to have a differential action on the two components which was statistically significant.5. The results are discussed in terms of depressant actions of the drugs on alpha-motorneurones, effects of the drugs at higher centres concerned with motor function, and the lack of evidence that spinal interneurones represent a specific site of action for centrally acting skeletal muscle relaxants.

Animals↗
PubMed1969

Post-tetanic and drug-induced repetitive firing in the soleus muscle of the cat.

1. The effects of a high frequency indirect tetanus on the responses to subsequent infrequently applied nerve shocks have been compared in the tibialis anterior and soleus muscles of cats and rabbits.2. Post-tetanic augmentation of twitches in the cat soleus muscle was shown to be partly due to repetitive firing and partly due to increased synchronization of the muscle fibre response. Post-tetanic repetitive firing was not evident in the responses of the other three muscles studied.3. Post-tetanic repetitive responses in the cat soleus muscle and nerve did not originate in the nerve trunk and were not produced by direct muscle stimulation; they were abolished by doses of tubocurarine smaller than those necessary to reduce the twitch tension below the pre-tetanic level. These findings support the conclusion of others that the repetitive firing originates at the neuromuscular junction.4. The repetitive firing could not be explained by an increase in the sensitivity of the motor endplates to acetylcholine, suggesting that an increase in and/or a prolongation of the output of transmitter from the motor nerve contributes to it.5. The cat soleus muscle was shown to be more sensitive to neostigmine than were the other three muscles studied, and acetylcholinesterase determinations showed that this muscle possesses less enzyme activity.6. It is concluded that an increase in transmitter output, coupled with a weaker cholinesterase activity, probably accounts for the post-tetanic repetitive activity in the cat soleus muscle.7. Post-tetanic repetitive firing was absent in cat soleus muscles which had been cross-innervated with the nerve formerly innervating a fast-contracting muscle.

Acetylcholine↗