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Iodophenpropit dihydrobromide

Names

[ CAS No. ]:
145196-87-8

[ Name ]:
Iodophenpropit dihydrobromide

[Synonym ]:
L-BMAA hydrochloride

Biological Activity

[Description]:

Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM)[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

H3 Receptor:0.32 nM (Kd)


[In Vitro]

Iodophenpropit is a very potent H3 receptor antagonist and shows only a moderate affinity for the H1 and H2 receptor[2]. Iodophenpropit inhibit 5-hydroxytryptamine (5-HT) responses with an IC50 of 1.57±0.3 μM[3].

[In Vivo]

Iodophenpropit (1 μg/kg; through intramuscular; b.i.d.; for 10 days) shows significant enhancement of total anti- sheep red blood cells (SRBC)- immunoglobulins (Igs) in rabbits[4]. Animal Model: New Zealand adult healthy rabbits of either sex weighing 1.63±0.36 kg[4] Dosage: 1 μg/kg Administration: Administered through intramuscular (i.m.); b.i.d.; for 10 days Result: Could influence a detectable antibody response to SRBC.

[References]

[1]. Jansen FP, et al. The first radiolabeled histamine H3 receptor antagonist, [125I]Iodophenpropit: saturable and reversible binding to rat cortex membranes. Eur J Pharmacol. 1992 Jul 7;217(2-3):203-5.

[2]. Leurs R, et al. Evaluation of the receptor selectivity of the H3 receptor antagonists, Iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed. Br J Pharmacol. 1995 Oct;116(4):2315-21.

[3]. Allen MC. Agonist and antagonist effects of histamine H3 receptor ligands on 5-HT3 receptor-mediated ion currents in NG108-15 cells. Eur J Pharmacol. 1998 Nov 20;361(2-3):261-8.

[4]. Trivendra Tripathi, et al. In vivo immunomodulatory profile of histamine receptors (H1, H2, H3 and H4): a comparative antagonists study. Asian Pac J Trop Med. 2010 Jun;3(6):465-470.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H21Br2IN4S

[ Molecular Weight ]:
576.13200

[ Exact Mass ]:
573.89000

[ PSA ]:
89.86000

[ LogP ]:
5.85400

Related Compounds