Talk:H2 antagonist

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--Inverse Agonist?-- I can't find a reference in my collection for h2-receptor antags being inverse agonists - Rang, Dale, Ritter Pharmacology 4th ed say its an competitive antagonist, I asked a clinical pharmacist about it and she thought I was smoking crack. A lecturer in clinical pharmacology at [Westmead Hospital], Chris Liddle said in a lecture delivered this year (2006) that it is a competitive antagonist. So if anyone cannot show otherwise I propose we remove the text.

--Barquinho 17:05, 17 May 2007 (UTC) It is likely that the sources given above refer to physiological systems in which constitutive activity of the receptor is absent or very low. In such cases an inverse agonist will behave as simple competitive antagonists. See Kenakin, T (2004) Mol Pharmacol 65:1-12 for a brief review on the general subject.
For examples of histamine H₂-receptor antagonists showing inverse agonist activity see:
Smith M et al. (1996) Proc Nat Acad Sci USA 93: 913-920; and
Monczor F et al. Mol Pharmacol 64: 512-520.

[edit] update risks

The latest medscape (2007/09/05) is carrying the following story:

"A study in the August Journal of the American Geriatrics Society found that long-term use of histamine-2 receptor antagonists (H2As) for gastric acid reflux and gastric ulcers may increase the risk of cognitive impairment in later life in African Americans"

Should this information be added?

Dilkie 16:40, 5 September 2007 (UTC)

Without reading the paper i would say that i shouldn't be included in this article. Subjects like the potential to cause cognitive impairment are difficult to interpret. I think with something like receptor pharmacology it is best to wait until the theory reaches the text book to add it to wikipedia.Dylan2106 (talk) 23:11, 7 January 2008 (UTC)

[edit] burimamine

I think there should be a bit more made of J Black's discovery of burimamide as a H2 competitive antagonist. The original paper, Definition and antagonism of histamine H 2 -receptors, J W Black et al Nature 1972 vol. 236 (5347) pp. 385-90 is a great read and really illustrates the practical application of Schild pharmacokinetic theory. Dylan2106 (talk) 23:15, 7 January 2008 (UTC

this gives a account of the development of the first H2 antagonists if anyone is interested. The account starts at around page 62. --Dylan2106 (talk) 17:27, 8 January 2008 (UTC)