New Class of Selective Stimulants of β-Adrenergic Receptors

Hartley, David J.; Jack, David; Lunts, L. H. C.; Ritchie, Alexander C.

doi:10.1038/219861a0

Cited by 87 publications

(34 citation statements)

References 6 publications

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“…This includes therapeutics with established efficacy in human disease (β 2 adrenoceptor agonists, anticholinergics, PDE inhibitors, steroids, cysLT 1 recceptor antagonists, 5-lipoxygenase/five lipoxygenase activating protein (FLAP) inhibitors) and therapeutics with modest or no beneficial effects in human disease, including anti-IL-5 antibodies, anti-TNF antibodies, and bradykinin, histamine, thromboxane and PAF receptor antagonists [9,10,20,21,35 -197,204,271-278]. A notable exception to this has been the many reports in guinea pigs showing beneficial effects of neurokinin receptor antagonists (see below).…”

Section: Therapeutic Interventions In Experimental Challengesmentioning

confidence: 99%

“…Many fundamental processes, mediators and regulators of airways disease pathogenesis were discovered or demonstrated first in guinea pigs, including the Schultz-Dale (immediate type hypersensitivity) reaction, the actions of histamine, the cysteinyl-leukotrienes and their two receptors, beta adrenoceptor subtypes, thromboxane, vascular endothelial growth factor (VEGF), eotaxin, alveolar macrophage derived neutrophil chemotactic factor(s) (leukotriene B 4 and/or IL-8) and the roles of cAMP and inositol triphosphate in signal transduction [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19]. Receptor pharmacology in guinea pigs more closely matches that of human receptor pharmacology than most other commonly used species [1,20,21] (Table 1, Figs.…”

Section: Introductionmentioning

confidence: 99%

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Using guinea pigs in studies relevant to asthma and COPD

Canning

Chou

2008

Pulmonary Pharmacology & Therapeutics

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The guinea pig has been the most commonly used small animal species in preclinical studies related to asthma and COPD. The primary advantages of the guinea pig are the similar potencies and efficacies of agonists and antagonists in human and guinea pig airways and the many similarities in physiological processes, especially airway autonomic control and the response to allergen. The primary disadvantages to using guinea pigs are the lack of transgenic methods, limited numbers of guinea pig strains for comparative studies and a prominent axon reflex that is unlikely to be present in human airways. These attributes and various models developed in guinea pigs are discussed.

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Section: Therapeutic Interventions In Experimental Challengesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Using guinea pigs in studies relevant to asthma and COPD

Canning

Chou

2008

Pulmonary Pharmacology & Therapeutics

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“…1) is a new bronchodilator chemically related to salbutamol. It has been shown to be 1.5 times more active than salbutamol in antagonizing the bronchoconstrictor action of acetylcholine in the anaesthetized guinea-pig, and to produce a similar increase in the contraction rate and isometric tension of guinea-pig isolated atria (Hartley, Jack, Lunts & Ritchie, 1968). At present the drug is only available for clinical trial.…”

Section: Introduction Methodsmentioning

confidence: 99%

The Clinical Pharmacology of Salmefamol

Evans¹,

Shenfield²,

Paterson³

1974

Brit J Clinical Pharma

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1 The absorption, excretion and metabolism of [3H] -salmefamol, a new sympathomimetic bronchodilator drug, have been studied in asthmatic patients. 2 Following oral administration of 1 or 2 mg to four patients the drug was well absorbed, peak plasma levels occurring from 0.6-2.0 h after administration. An improvement in forced expiratory volume in 1 s (FEV1) (ranging from 12-50% above baseline) was seen. 3 Following aerosol administration of 0.22-0.34 mg to four patients a rapid rise in FEV1 was seen (range 26-117%). The plasma and urinary pictures following this route were similar to those seen after oral administration, suggesting that the majority of the dose was swallowed. 4 Very little free salmefamol was found in plasma or urine, the majority being present as metabolites. Urinary radioactivity was mainly present in the form of sulphate conjugates of at least two compounds, one of which was salmefamol. The other compound has not been identified but it is suggested that it may be an active metabolite.

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“…The present work confirms the superiority of salmefamol over salbutamol using spirometric tests performed in the laboratory. This longer action of salmefamol is possibly due to the fact that one of its pre-conjugation metabolites, AH4553, possesses bronchodilator properties (Hartley, Jack, Lunts & Ritchie, 1968;Evans, Shenfield & Paterson, 1974).…”

Section: Patientsmentioning

confidence: 99%

Comparison of salmefamol and salbutamol in patients with chronic airways obstruction.

Iw¹,

Dash²,

McHardy³

et al. 1976

Brit J Clinical Pharma

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1 Inhaled salmefamol, in doses of 100 mug and 200 mug has been compared with inhaled salbutamol, in a dose of 200 mug, and with placebo in patients with airways obstruction. 2 Both salmefamol and salbutamol are potent bronchodilators with a signficantly superior action over placebo at all times up to 8 h after treatment. 3 The mean peak percentage increases in FEV produced by the three active preparations were similar. The decline from peak values was significantly slower with salmefamol than with salbutamol. Neither drug produced tachycardia.

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New Class of Selective Stimulants of β-Adrenergic Receptors

Cited by 87 publications

References 6 publications

Using guinea pigs in studies relevant to asthma and COPD

Using guinea pigs in studies relevant to asthma and COPD

The Clinical Pharmacology of Salmefamol

Comparison of salmefamol and salbutamol in patients with chronic airways obstruction.

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