U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 201 - 210 of 1608 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


1-Methylhistamine also known as tele-methylhistamine can be found primarily in most biofluids, including cerebrospinal fluid (CSF), urine, feces, and blood, as well as in human bone marrow, brain, and mast cell tissues; it is involved in histidine metabolism. This endogenous compound can be a marker of the inflammatory bowel disease because during the development of the disease it concentration is enhanced. Besides, experiments on dogs have revealed, that 1-methylhistamine can be used as a marker of intestinal inflammation in chronic gastrointestinal disease.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Thioperamide is an antihistamine at H3 and H4 receptors. Thioperamide behaves as both antagonist and inverse agonist.Thioperamide is under preclinical development with Glaxo Wellcome (UK) for the treatment of short-term memory impairment. It has also demonstrated antiarrhythmic effects in preclinical trials. Active development of thioperamide appears to have been discontinued.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Imetit (S-[2-(4-(imidazolyl)ethyl]isothiourea) is a highly specific and potent histamine H3 receptor agonist. It is widely used to study H3-mediated signaling.
Zolantidine is the novel benzthiazole derivative. It is a centrally acting potent antagonist of histamine at H2-receptors. It was found to be a competitive inhibitor of the histamine catabolising enzyme in brain, histamine N-methyltransferase. High aggression in histamine N-methyltransferase knockout mice was suppressed by treatment with zolantidine, indicating that abnormal histamine H2 receptor activation promoted aggression in knockout mice. Histamine H(3) receptor antagonist JNJ-10181457-induced anxiety-like behaviours were dominantly reduced by zolantidine. Zolantidine significantly attenuated the discriminative stimulus effects of morphine.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

alpha-N-methyl-histamine is a metabolite of histamine that plays an important role in several (patho) physiological processes. alpha-N-methyl-histamine is being a potent agonist of histamine H3 receptor can be used as an effective therapeutic alternative in migraine patients.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ 7777120) is the first selective antagonist of the histamine H4 receptor. Johnson & Johnson Pharmaceutical Research and Development is developing JNJ 7777120 for the treatment of inflammatory disorders. JNJ 7777120 demonstrates efficacy as anti-inflammatory agents in vivo. JNJ 7777120 have shown promising activity in down-regulating immune responses in a range of animal disease models including acute inflammation, hapten-mediated colitis, allergic airway inflammation (e.g. allergic rhinitis), colitis, allergic pruritis and atopic dermatitis.