TY - JOUR
T1 - Pharmacological Profile of New Histamine H2‐Receptor Antagonists Related to Cimetidine, Ranitidine and Lamtidine
AU - Orsetti, M.
AU - Sorba, G.
PY - 1988/1
Y1 - 1988/1
N2 - Abstract— New compounds structurally related to cimetidine, ranitidine and lamtidine have been prepared and tested for their histamine H2‐receptor blocking activity on guinea‐pig atria, rat perfused stomach and frog isolated gastric mucosa. These derivatives contain as a polar group, a diaminofurazan moiety, a 3‐amino‐4‐methylfurazan or a 3‐amino‐4‐phenylfurazan moiety. Ranitidine and lamtidine analogues display strong H2‐antagonist activity in‐vitro (KB on atria 0.037 μM and 0.0039 μM, respectively) and in‐vivo on the lumen‐perfused stomach of the anaesthetized rat (ID50 0.13 μmol kg−1 and 0.023 μmol kg−1 i.v., respectively). However, lamtidine analogues are ineffective in blocking the histamine‐induced increase of H+ output in the frog isolated gastric mucosa. On the basis of the anomalous results in the frog, it is concluded that caution must be exercised in extrapolating information from amphibian to mammalian tissues with regard to the structure and the function of histamine receptors. 1988 Royal Pharmaceutical Society of Great Britain
AB - Abstract— New compounds structurally related to cimetidine, ranitidine and lamtidine have been prepared and tested for their histamine H2‐receptor blocking activity on guinea‐pig atria, rat perfused stomach and frog isolated gastric mucosa. These derivatives contain as a polar group, a diaminofurazan moiety, a 3‐amino‐4‐methylfurazan or a 3‐amino‐4‐phenylfurazan moiety. Ranitidine and lamtidine analogues display strong H2‐antagonist activity in‐vitro (KB on atria 0.037 μM and 0.0039 μM, respectively) and in‐vivo on the lumen‐perfused stomach of the anaesthetized rat (ID50 0.13 μmol kg−1 and 0.023 μmol kg−1 i.v., respectively). However, lamtidine analogues are ineffective in blocking the histamine‐induced increase of H+ output in the frog isolated gastric mucosa. On the basis of the anomalous results in the frog, it is concluded that caution must be exercised in extrapolating information from amphibian to mammalian tissues with regard to the structure and the function of histamine receptors. 1988 Royal Pharmaceutical Society of Great Britain
UR - http://www.scopus.com/inward/record.url?scp=0023857480&partnerID=8YFLogxK
U2 - 10.1111/j.2042-7158.1988.tb05145.x
DO - 10.1111/j.2042-7158.1988.tb05145.x
M3 - Article
SN - 0022-3573
VL - 40
SP - 31
EP - 34
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
IS - 1
ER -