Comparative Action of the Lanthanides and D-600 on Smooth Muscle Contraction

Triggle, Christopher R.; Swamy, Vinushree; Ticku, R.; Triggle, D.J.

doi:10.1016/b978-0-08-021308-8.50129-0

Cited by 5 publications

(7 citation statements)

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“…Native calcium channels bind calcium channel blockers stereospecifically (Ferry and Glossmann, 1982;Triggle and Swamy, 1983), which is observed in experiments in which increasing concentrations of the (+) and (-) enantiomers of a blocker are added to a binding assay carried out at subsaturating concentrations of [3H]isradipine. Figure 2b demonstrates that the newly expressed a1 subunit binds the (+) enantiomer of isradipine with -100-fold higher affinity than the (-) enantiomer.…”

Section: Resultsmentioning

confidence: 99%

Stable and functional expression of the calcium channel alpha 1 subunit from smooth muscle in somatic cell lines.

et al. 1992

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Voltage‐activated calcium channels are membrane spanning proteins that allow the controlled entry of Ca2+ into the cytoplasm of cells. The principal channel forming subunit of an L‐type calcium channel is the alpha 1 subunit. Transfection of Chinese hamster ovary (CHO) cells with complementary DNA encoding the calcium channel alpha 1 subunit from smooth muscle led to the expression of functional calcium channels which bind calcium channel blockers and show the voltage‐dependent activation and slow inactivation and unitary current conductance characteristic of calcium channels in smooth muscle. The currents mediated by these channels are sensitive towards dihydropyridine‐type blockers and agonists indicating that the calcium channel blocker receptor sites were present in functional form. The smooth muscle alpha 1 subunit cDNA alone is sufficient for stable expression of functional calcium channels with the expected kinetic and pharmacological properties in mammalian somatic cells.

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Section: Resultsmentioning

confidence: 99%

Stable and functional expression of the calcium channel alpha 1 subunit from smooth muscle in somatic cell lines.

et al. 1992

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“…The potency of an agonist is a function of many factors, the affinity and efficacy being major determinants of the stimulus to produce the response (Jenkinson, 1973;Triggle & Triggle, 1976). The possibility exists that the exchange between salbutamol and fenoterol arises from efficacy differences.…”

Section: Discussionmentioning

confidence: 99%

“…However, this measure is not sufficient for characterization of the receptors by the use of agonists, the individual contributions of both the affinity (measured as the dissociation constant) and the relative efficacy must be determined (Jenkinson, 1973: Triggle & Triggle, 1976 Brink, 1973;Buckner & Saini, 1975). In the present paper we have applied the latter method to several full and partial agonists at f-adrenoceptors of isolated left and right guinea-pig atria and have extended it to determine additionally their relative efficacies.…”

Section: Introductionmentioning

confidence: 99%

Functional Antagonism as a Means of Determining Dissociation Constants and Relative Efficacies of Sympathomimetic Amines in Guinea‐pig Isolated Atria

Broadley

Nicholson

1979

British J Pharmacology

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I The positive inotropic and chronotropic responses to sympathomimetic amines were examined in guinea-pig isolated atria.2 The order of potency measured from EC3o values was isoprenaline > orciprenaline > salbutamol > fenoterol > terbutaline. Terbutaline and salbutamol were partial agonists on rate and together with orciprenaline and fenoterol also on tension responses. 3 Functional antagonism by carbachol caused a rightwards shift of the dose-response curve and depression of the maximum response. The rate maxima for orciprenaline, fenoterol and terbutaline were above that of isoprenaline. All the tension maxima were below isoprenaline. 4 Dissociation constants (KA) and relative efficacies (er) were determined by analogy with irreversible antagonism. 5 The relative orders of affinity (KA) were isoprenaline > orciprenaline > fenoterol > salbutamol > terbutaline. Affinities were identical on rate and tension. 6 The relative efficacies were all greater than isoprenaline for rate responses. On tension they were the same or less than isoprenaline. 7 The implications of these results are discussed, in particular the fact that a partial agonist has a greater efficacy than a full agonist.

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“…Some pharmacological activities exhibited by DHPs include antihypertensive, antianginal, antitumor, anti‐flammatory, antitubercular, analgesic and antithrombotic ,,. They also exhibit other activities like calcium channel antagonists, vasodilation, anticonvulsant, stress protective effect and cardio depressant activity ,…”

Section: Introductionmentioning

confidence: 99%

Bis{cis‐[MoO₂]} Complexes of 4,6‐Diacetyl Resorcinol Bis(hydrazone)and Their Catalytic Application for the Three Components Dynamic Covalent Assembly via Hantzsch Reaction

et al. 2017

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= 4,6-diacetyl resorcinol and Hbhz = benzoylhydrazide, Hinh = isonicotinoylhydrazide, Hnah = nicotinoylhydrazide, and Hfah = 2-furoylhydrazide) have been prepared by the reaction of ligand with [Mo VI O 2 (acac) 2 ] (Hacac = acetylacetone) in 1:2 ratio in methanol. Isolated complexes(4) are characterized by elemental (CHN) analysis, spectral (FT-IR, UV-vis, 1 H and 13 C NMR) and thermogravimetric analysis.Single crystal X-ray diffraction analysis of complexes 1, 2 and 4 confirms their binuclear structure and distorted octahedral geometry around each molybdenum where ligands behave as bis(dibasic tridentate) coordinating through phenolic oxygen, azomethine nitrogen and enolic oxygen atoms of each unit. These complexes have successfully been used as catalyst precursors in solvent as well as solvent free conditions for the one-pot three components (ethylacetoacetate, benzaldehyde and ammonium acetate) dynamic covalent assembly, via Hantzsch reaction using hydrogen peroxide as an oxidant.

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Comparative Action of the Lanthanides and D-600 on Smooth Muscle Contraction

Cited by 5 publications

References 0 publications

Stable and functional expression of the calcium channel alpha 1 subunit from smooth muscle in somatic cell lines.

Stable and functional expression of the calcium channel alpha 1 subunit from smooth muscle in somatic cell lines.

Functional Antagonism as a Means of Determining Dissociation Constants and Relative Efficacies of Sympathomimetic Amines in Guinea‐pig Isolated Atria

Bis{cis‐[MoO₂]} Complexes of 4,6‐Diacetyl Resorcinol Bis(hydrazone)and Their Catalytic Application for the Three Components Dynamic Covalent Assembly via Hantzsch Reaction

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Comparative Action of the Lanthanides and D-600 on Smooth Muscle Contraction

Cited by 5 publications

References 0 publications

Stable and functional expression of the calcium channel alpha 1 subunit from smooth muscle in somatic cell lines.

Stable and functional expression of the calcium channel alpha 1 subunit from smooth muscle in somatic cell lines.

Functional Antagonism as a Means of Determining Dissociation Constants and Relative Efficacies of Sympathomimetic Amines in Guinea‐pig Isolated Atria

Bis{cis‐[MoO2]} Complexes of 4,6‐Diacetyl Resorcinol Bis(hydrazone)and Their Catalytic Application for the Three Components Dynamic Covalent Assembly via Hantzsch Reaction

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Bis{cis‐[MoO₂]} Complexes of 4,6‐Diacetyl Resorcinol Bis(hydrazone)and Their Catalytic Application for the Three Components Dynamic Covalent Assembly via Hantzsch Reaction