Thioperamide - CAS 106243-16-7
Category: Inhibitor
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Histamine Receptor
Thioperamide is a potent histamine H3 and H4 antagonist/inverse agonist (Ki = 25 and 27 nM for human recombinant H3 and H4 receptors, respectively). Thioperamide can cross the blood-brain barrier freely.
Brife Description:
histamine H3/H4 antagonist
≥99% by HPLC
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1.Histamine H(3) receptor modulates nociception in a rat model of cholestasis.
Hasanein P Pharmacol Biochem Behav. 2010 Sep;96(3):312-6. doi: 10.1016/j.pbb.2010.05.023. Epub 2010 Jun 1.
Cholestasis is associated with changes including analgesia. The histaminergic system regulates pain perception. The involvement of histamine H(3) receptors in modulation of nociception in a model of elevated endogenous opioid tone, cholestasis, was investigated in this study using immepip and thioperamide as selective H(3) receptor agonist and antagonist respectively. Cholestasis was induced by ligation of main bile duct using two ligatures and transsection the duct between them. Cholestatic rats had increased tail-flick latencies (TFLs) compared to non-cholestatics. Administration of immepip (5 and 30mg/kg) and thioperamide (10 and 20mg/kg) to the cholestatic groups significantly increased and decreased TFLs compared to the saline treated cholestatic group. Immepip antinociception in cholestatic animals was attenuated by co-administration of naloxone. Immepip and thioperamide injections into non-cholestatic animals did not alter TFLs. At the doses used here, none of the drugs impaired motor coordination, as revealed by the rotarod test. The present data show that the histamine H(3) receptor system may be involved in the regulation of nociception during cholestasis in rats.
2.Cytokine responses of intraepithelial lymphocytes are regulated by histamine H(2) receptor.
Takagaki K;Osawa S;Horio Y;Yamada T;Hamaya Y;Takayanagi Y;Furuta T;Hishida A;Ikuma M J Gastroenterol. 2009;44(4):285-96. doi: 10.1007/s00535-009-0019-9. Epub 2009 Mar 10.
BACKGROUND: ;Histamine participates in the immune regulation of several gastrointestinal diseases. However, the effect of histamine on intestinal intraepithelial lymphocytes (IELs), the front line of the intestinal mucosal immune system, is not well understood. We examined whether histamine has a direct effect on cytokine production by IELs and the involvement of histamine receptor subtypes.;METHODS: ;Murine IELs were activated by PMA plus ionomycin with/without histamine. Secreted cytokines were measured and compared with those of splenocytes. Intracellular cytokines were detected by flow cytometry. Expression of histamine receptor subtypes in IELs was examined by RT-PCR.;RESULTS: ;Histamine H(1) receptor (H(1)R), H(2)R, and H(4)R, but not H(3)R mRNA were expressed on IELs. Histamine significantly decreased Th1-cytokine (IFN-gamma, TNF-alpha, and IL-2) and also IL-4 production in IELs as well as splenocytes. The selective H(2)R antagonist famotidine, but not the H(1)R antagonist pyrilamine nor the H(3)R/H(4)R antagonist thioperamide, competes with the inhibitory effect of histamine on these cytokine production in IELs. These suppressive effects of histamine were mimicked by a selective H(2)R/H(4)R agonist dimaprit.
3.Influence of imidazole replacement in different structural classes of histamine H(3)-receptor antagonists.
Meier G;Apelt J;Reichert U;Grassmann S;Ligneau X;Elz S;Leurquin F;Ganellin CR;Schwartz JC;Schunack W;Stark H Eur J Pharm Sci. 2001 Jun;13(3):249-59.
The reference compounds for histamine H(3)-receptor antagonists carry as a common feature an imidazole moiety substituted in the 4-position. Very recently novel ligands lacking an imidazole ring have been described possessing a N-containing non-aromatic heterocycle instead. In this study we investigated whether imidazole replacement, favourably by a piperidine moiety, is generally applicable to different structural classes of reference compounds, e.g., thioperamide, carboperamide, clobenpropit, FUB 181, ciproxifan, etc. While replacement led to a loss of affinity for many of the compounds, it was successfully applied to some ether derivatives. The piperidine analogues of FUB 181 and ciproxifan, 3-(4-chlorophenyl)propyl 3-piperidinopropyl ether hydrogen oxalate (6) and cyclopropyl 4-(3-piperidinopropyloxy)phenyl methanone hydrogen maleate (7), almost maintained in vitro affinities, pK(i) values of 7.8 and 8.4, respectively, and showed high potency in vivo after p.o. administration (ED(50) values of 1.6 and 0.18 mg/kg, respectively).
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CAS 106243-16-7 Thioperamide

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