Metiamide—An orally active histamine H2-receptor antagonist

Black, Joseph; Duncan, W. A. M.; Emmett, J. C.; Ganellin, C. Robin; Hesselbo, T.; Parsons, M E; Wyllie, J. H.

doi:10.1007/bf01986676

Cited by 5 publications

(2 citation statements)

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“…These observations have been extended using the selective H 1 ‐receptor antagonist, mepyramine and the selective H 2 ‐receptor antagonist, metiamide (Black, Duncan, Emmett, Ganellin, Hesselbo, Parsons & Wyllie, 1973) and the histamine depressor responses have been analyzed in terms of the receptors involved.…”

Section: Introductionmentioning

confidence: 99%

An analysis of the depressor responses to histamine in the cat and dog: involvement of both H₁‐ and H₂‐receptors

Black

Owen²,

Parsons³

2010

British J Pharmacology

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1 The depressor responses to histamine, in anaesthetized cats and dogs, have been shown to involve both histamine H1-and H2-receptors. 2 In both species, histamine caused dose-dependent falls in blood pressure. The dose-response curve could be displaced to the right by administration of mepyramine 2.5 ¥ 10 -6 mol/kg i.v. The displacement was maximal with a dose-ratio of less than ten. 3 Metiamide alone, up to 2 ¥ 10 -6 mol kg -1 min -1 , had no significant effect on the histamine dose-response curve. 4 When administered in the presence of mepyramine, metiamide, 4 ¥ 10 -7 and 2 ¥ 10 -6 mol kg -l min -l , caused dose-dependent displacements to the right, of the histamine dose-response curve greater than could be achieved with mepyramine alone. 5 The results indicate the presence of both histamine H1-and H2-receptors in the cardiovascular system of the cat and dog. Both receptors produce a common response, i.e. a fall in blood pressure.

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Section: Introductionmentioning

confidence: 99%

An analysis of the depressor responses to histamine in the cat and dog: involvement of both H₁‐ and H₂‐receptors

Black

Owen²,

Parsons³

2010

British J Pharmacology

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show abstract

Section: Introductionmentioning

confidence: 99%

AN ANALYSIS OF THE DEPRESSOR RESPONSES TO HISTAMINE IN THE CAT AND DOG: INVOLVEMENT OF BOTH H₁‐ AND H₂‐RECEPTORS

Black

Owen²,

Parsons³

1997

British J Pharmacology

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1 The depressor responses to histamine, in anaesthetized cats and dogs, have been shown t o involve both histamine HI -and H2-receptors.2 In both species, histamine caused dose-dependent falls in blood pressure. The dose-response curve could be displaced t o the right by administration of mepyramine 2.5 x 10-mol/kg i.v. The displacement was maximal with a dose-ratio of less than ten. 3 mol kg-' min-', had no significant effect on the histamine dose-response curve.4 mol kg-' min-I, caused dose-dependent displacements t o the right, of the histamine dose-response curve greater than could be achieved with mepyramine alone. 5The results indicate the presence of both histamine H I -and H2-receptors in the cardiovascular system of the cat and dog. Both receptors produce a common response, i.e. a fall in blood pressure.

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Novel Histamine H₃‐Receptor Antagonists with Benzyl Ether Structure or Related Moieties: Synthesis and Structure‐Activity Relationships

Hüls¹,

Purand²,

Stark³

et al. 1996

Archiv der Pharmazie

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In search of new histamine H3-receptor ligands sixteen ether derivatives of 3-(1H-imidazol-4-yl)propanol with benzylic partial structure or related moieties were prepared and investigated as H3-receptor antagonists. The new compounds belong to a general construction pattern developed by other histamine H3-receptor antagonists. Structural modifications were introduced in an attempt to optimize in vitro as well as in vivo activity. Structure-activity relationships of the new histamine H3-receptor antagonists are discussed. All ether derivatives showed in vitro activities in the nanomolar concentration range, but only compounds with bulky lipophilic residues were also active under in vivo conditions. The most active compound within this series was 3-(1H-imidazol-4-yl)propyl 1-naphthylmethyl ether (4n) presenting an ED50 of 3.2 +/- 1.9 mg/kg regarding enhancement of endogenous histamine in brain after p.o. administration to mice. Furthermore, comparison of the H3-receptor activities measured on synaptosomes of rat cerebral cortex and on guinea pig ileum gave a good correlation indicating homogeneity of central and peripheral H3-receptor test models. The most interesting compounds were also evaluated in functional in vitro assays with regard to their activities at histamine H1-, H2-, and muscarinic M3-receptors. The tested compounds showed very weak activities at these receptor subtypes demonstrating their H3-receptor selectivity.

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Metiamide—An orally active histamine H2-receptor antagonist

Cited by 5 publications

References 2 publications

An analysis of the depressor responses to histamine in the cat and dog: involvement of both H₁‐ and H₂‐receptors

An analysis of the depressor responses to histamine in the cat and dog: involvement of both H₁‐ and H₂‐receptors

AN ANALYSIS OF THE DEPRESSOR RESPONSES TO HISTAMINE IN THE CAT AND DOG: INVOLVEMENT OF BOTH H₁‐ AND H₂‐RECEPTORS

Novel Histamine H₃‐Receptor Antagonists with Benzyl Ether Structure or Related Moieties: Synthesis and Structure‐Activity Relationships

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Metiamide—An orally active histamine H2-receptor antagonist

Cited by 5 publications

References 2 publications

An analysis of the depressor responses to histamine in the cat and dog: involvement of both H1‐ and H2‐receptors

An analysis of the depressor responses to histamine in the cat and dog: involvement of both H1‐ and H2‐receptors

AN ANALYSIS OF THE DEPRESSOR RESPONSES TO HISTAMINE IN THE CAT AND DOG: INVOLVEMENT OF BOTH H1‐ AND H2‐RECEPTORS

Novel Histamine H3‐Receptor Antagonists with Benzyl Ether Structure or Related Moieties: Synthesis and Structure‐Activity Relationships

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Product

Resources

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An analysis of the depressor responses to histamine in the cat and dog: involvement of both H₁‐ and H₂‐receptors

An analysis of the depressor responses to histamine in the cat and dog: involvement of both H₁‐ and H₂‐receptors

AN ANALYSIS OF THE DEPRESSOR RESPONSES TO HISTAMINE IN THE CAT AND DOG: INVOLVEMENT OF BOTH H₁‐ AND H₂‐RECEPTORS

Novel Histamine H₃‐Receptor Antagonists with Benzyl Ether Structure or Related Moieties: Synthesis and Structure‐Activity Relationships