Spasmogenic activity

Spasmogenic activity. Ethanol (95%) extract of the fresh leaf and stem, administered to guinea pigs at a dose of 0.5 mL/L, was active on ileum. Water extract of the fresh leaf and stem, administered intraperi-toneally to guinea pigs at a dose of 0.5 mL/L, was active on ileum . 

Serum HDL-lowering effect. Seed fixed oil, administered to male hamsters at a concentration of 19% of diet, was inactive Serum LDL-lowering effect Seed oil, administered orally to male adults at a dose of 30.5% of diet, produced weak activity ". Spasmogenic activity. Water extract of the dried leaf, administered to rats at a dose of 0.1 pg/mL was active on ileum and a dose of 0.3 pg/mL was active on ileum vs acetylcholine-induced contractions ... 

Radical scavenging effect. Seed oil, in cell culture, was active on astrocytes vs peroxide radical scavenging, IC50 27461 ppm . Spasmogenic activity. Methanol (70%) extract of the seed, administered to guinea pigs at a dose of 1 mg/mL, was active on the uterus and ileum. The effect was abolished... 

The spasmogenic activity of 93a and 93b was identified as an indirect cholinergic action. Additionally both esters exhibit a weak anticholinergic and a weak noncompetitive papaverine-like action. Great differences between 93a and 93b were not observed. 

In the guinea-pig ileum bioassay, extracts and homogenates of S. mansoni produce spasmogenic activity this activity is abolished with cholinesterase treatment or blocked... 

Anaphylatoxins The family of peptides C3a, C4a, C5a, and C5a des-arginine produced in the serum during complement activation. They produce smooth muscle contraction, mast cell histamine release, affect platelet aggregation, and act as mediators of the local inflammatory process. The order of anaphylatoxin activity from strongest to weakest is C5a, C3a, C4a, and C5a des-arginine. The latter is the so-called "classical" anaphylatoxin but shows no spasmogenic activity though it contains some chemotactic ability, [nih]... 

Ergot alkaloids (ergotamine, ergonovine) also exhibit certain nonselective a-adrenoblocking activity however, they primarily exhibit spasmogenic action on smooth muscle, causing a constriction of blood vessels. 

In contrast to many other smooth muscle types, ASM is regarded as being multi-unit rather than single unit, which means that each smooth muscle cell is individually innervated. This is associated with a relative lack of gap junctions which normally provide a low resistance electrical pathway for cell to cell communication. Spontaneous electrical activity is rarely observed in ASM cells and action potentials only occur in exceptional circumstances, the usual electrical response to spasmogens being graded depolarization without the overall muscle bundle acting as a syncytium. 

The second messenger linking activation of surfece receptors by spasmogens in smooth muscle to release of intracellular Ca " has been identified as IP3. IP3 is formed by activated receptor stimulation of a cell membrane enzyme, PLC, which hydrolyses a lipid constituent of the cell membrane, phosphatidylinositol bisphosphate (PIP2 Fig. 9.4). 

PG 15 (R) 15-me—E2me ester inhibitor gastric secretion spasmogen smooth muscle prolonged action active at oral administration... 

ML antispasmodic activities are inhibition of the contraction of intestine using cholinomimetic as spasmogen. 

Chloroform extracts of dried feverfew leaves produced reversible constructions of vascular smooth muscle, while ones of fresh leaves caused an irreversible, non-specific inhibition of contractility. It is shown that chloroform extracts contain substances which inhibit voltage-dependent K+ currents by an open channel-blocking mechanism. This effect could account for the spasmogenic action and antimigraine activity, and be related to the lactone content [154,215,229]. 

EXTRAVASCULAR SMOOTH MUSCLE Histamine stimulates or, more rarely, relaxes various extravascular smooth muscles. Contraction is due to activation of H j receptors (linked to and Ca + mobilization) relaxation (for the most part) is due to activation of Hj receptors. Minute doses of histamine will evoke intense bronchoconstriction in patients with bronchial asthma and certain other pulmonary diseases. Although the spasmogenic influence of Hj receptors is dominant in bronchial muscle, receptors with dilator function also are present. Thus, histamine-induced bronchospasm is potentiated slightly by blockade. 

Ethanol and aqueous extracts of B. crassifolia bark have also been reported to have good anti-inflammatory activity in the HET-CAM and the cyclooxygenase inhibition assays as well as antimicrobial activity [86, 87, 88]. In addition, we reported that the leaf and bark extracts of B. crassifolia displayed concentration-dependent, spasmogenic effects on rat... 

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