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Restrict the search for
histamine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
A-987306 is a new histamine H(4) antagonist. A-987306 is potent in H(4) receptor binding assays (rat H(4), K(i) = 3.4 nM, human H(4) K(i) = 5.8 nM) and demonstrated potent functional antagonism in vitro at human, rat, and mouse H(4) receptors in cell-based FLIPR assays. A-987306 also demonstrated H(4) antagonism in vivo in mice, blocking H(4)-agonist induced scratch responses, and showed anti-inflammatory activity in mice in a peritonitis model. Most interesting was the high potency and efficacy of this compound in blocking pain responses, where it showed an ED(50) of 42 umol/kg (ip) in a rat post-carrageenan thermal hyperalgesia model of inflammatory pain. A-987306 inhibited the scratching response (IC50 = 0.4 umoles/kg, i.p.) with (85%) inhibition seen at 30 umoles/kg, i.p. A-987306 is a potent and selective H4R antagonist with robust antipruritic activity and is a useful tool for further exploration of the role of H4R receptors in vivo.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
A-943931 is a potent and selective H4R antagonist with high affinity at both human (Kis = 4.6 nM) and rat (Kis = 3.8 nM) receptors. A-943931 competitively and potently antagonizes rat H4R agonist-mediated responses in [35S]GTPγS binding assays (Kbs = 28 nM) and intracellular calcium mobilization at rat and human receptors (Kbs from 5-10 nM). When tested in vivo in a mouse model of clobenpropit (10 nM, i.d.) induced scratching, A-943931 inhibited the scratching response (IC50 = 26 umoles/kg, i.p.) with significant inhibition (69%) at the highest tested dose (30 umoles/kg, i.p.). A-943931 is a potent and selective H4R antagonist with robust antipruritic activity and is a useful tool for further exploration of the role of H4R receptors in vivo.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
ABT-239 is a selective, nonimidazole H3 receptor antagonist/inverse agonist, which was investigated by Abbott laboratory as a potential drug for treatment of a variety of cognitive disorders including attention deficit/hyperactivity disorder, Alzheimer's disease, and schizophrenia.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at human (pKi=9.24) H3 receptor and was developed by Johnson & Johnson Pharmaceutical. During preclinical studies were shown that JNJ-5207852 might be useful in the treatment of cognitive impairment in epilepsy. On animal models was discovered, that this compound readily penetrates the brain tissue after subcutaneous administration.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
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)
Targets:
Conditions:
JNJ-10181457 is a histamine H3 receptor antagonist, which was developed by Johnson & Johnson. Selective blockade of histamine H3 receptors might have therapeutic utility for the treatment of working memory deficits and learning disorders, especially those in which ACh neurotransmission is compromised.
