Aminopotentidine - CAS 140873-26-3
Category: Inhibitor
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Histamine Receptor
Aminopotentidine is a high selectivity and high affinity histamine H2 receptor antagonist. Its KB values are 220 and 280 nM at human and guinea pig H2 receptors respectively. It is the precursor for the synthesis of the [125I]-iodo derivative, so it can be used in the synthetic preparation of an iodo derivative.
≥97% by HPLC
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1.Cardiac and gastric effects of histamine H2 receptor antagonists: no evidence for a correlation between lipophilicity and receptor affinity.
Coruzzi G;Adami M;Pozzoli C;Giorgi F;Bertaccini G Br J Pharmacol. 1996 Aug;118(7):1813-21.
1. A series of histamine H2 receptor antagonists with different lipophilicity were tested in cardiac and gastric assays in order to reveal possible differences in receptor affinity. Lipophilicity of the compounds was expressed as CLOG P (theoretically-determined logarithm of octanol:water partition coefficient) and log k' (logarithm of capacity factor, experimentally-determined by reverse-phase high performance liquid chromatography). 2. Aminopotentidine (APT) and iodoaminopotentidine (I-APT), which are both lipophilic compounds, behaved as insurmountable antagonists of histamine responses in rat isolated gastric fundus (pKB = 6.20 +/- 0.16 and 6.89 +/- 0.19, respectively) and guinea-pig isolated papillary muscle (pKB = 6.34 +/- 0.37 and 6.81 +/- 0.26, respectively). They were approximately as effective as ranitidine (RAN) in reducing histamine-induced acid secretion in the anaesthetized rat, ID50 values being 0.018 +/- 0.02, 0.020 +/- 0.03 and 0.036 +/- 0.01 mumol kg-1 i.v. for APT, I-APT and RAN, respectively. Both APT and I-APT had a significantly longer duration of action than RAN. 3. The hydrophilic compound, SK&F 92857, was inactive up to 10 microM in modifying histamine-induced acid secretion in the isolated rat stomach.
2.The pharmacological activity of some new fluorescent small molecule histamine H2 receptor (H2-R) ligands, derived from aminopotentidine and squaramide, in the GTPase assay.
Petrache G;Pavelescu MD Rev Med Chir Soc Med Nat Iasi. 2010 Jan-Mar;114(1):255-9.
We characterized the pharmacological activity of some new fluorescent and nonfluorescent ligands derived from aminopotentidine and squaramide with respect to the interaction with human (h) and guinea pig (gp) H2R species isoforms on Spodoptera frugiperda (Sf9) cell membranes expressing H2R-Gsalpha fusion proteins.;MATERIAL AND METHOD: ;The pharmacological studies were performed in a radioactivity-based GTPase assay. Non-linear curve ?tting was performed using the computer program Prism 4.0 (GraphPad-Prism).;RESULTS: ;Interestingly is that the aminopotentidine ligands labeled with S0536 dye showed a higher activity than the squaramide ligands labeled with the same fluorophor. Moreover, for some cases, the bulky fluorescent groups can even substantially increase ligand affinity.;CONCLUSION: ;The study of comparative antagonist activity of new H2R ligands derived from aminopotentidine and squaramide in the GTPase assay suggests that there is no common, lock' for all, keys' at the H2R.
3.Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Beukers MW;Klaassen CH;De Grip WJ;Verzijl D;Timmerman H;Leurs R Br J Pharmacol. 1997 Nov;122(5):867-74.
1. Rat histamine H2 receptors were epitope-tagged with six histidine residues at the C-terminus to allow immunological detection of the receptor. Recombinant baculoviruses containing the epitope-tagged H2 receptor were prepared and were used to infect insect Sf9 cells. 2. The His-tagged H2 receptors expressed in insect Sf9 cells showed typical H2 receptor characteristics as determined with [125I]-aminopotentidine (APT) binding studies. 3. In Sf9 cells expressing the His-tagged H2 receptor histamine was able to stimulate cyclic AMP production 9 fold (EC50=2.1+/-0.1 microM) by use of the endogenous signalling pathway. The classical antagonists cimetidine, ranitidine and tiotidine inhibited histamine induced cyclic AMP production with Ki values of 0.60+/-0.43 microM, 0.25+/-0.15 microM and 28+/-7 nM, respectively (mean+/-s.e.mean, n=3). 4. The expression of the His-tagged H2 receptors in infected Sf9 cells reached functional levels of 6.6+/-0.6 pmol mg(-1) protein (mean+/-s.e.mean, n=3) after 3 days of infection. This represents about 2 x 10(6) copies of receptor/cell. Preincubation of the cells with 0.03 mM cholesterol-beta-cyclodextrin complex resulted in an increase of [125I]-APT binding up to 169+/-5% (mean+/-s.
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CAS 140873-26-3 Aminopotentidine

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