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145196-87-8

145196-87-8 structure
145196-87-8 structure
  • Name: Iodophenpropit dihydrobromide
  • Chemical Name: 3-(1H-Imidazol-4-yl)propyl N-[2-(4-iodophenyl)ethyl]carbamimidoth ioate dihydrobromide
  • CAS Number: 145196-87-8
  • Molecular Formula: C15H21Br2IN4S
  • Molecular Weight: 576.13200
  • Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
  • Create Date: 2016-01-24 07:34:58
  • Modify Date: 2024-01-08 10:25:06
  • 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].

Name 3-(1H-Imidazol-4-yl)propyl N-[2-(4-iodophenyl)ethyl]carbamimidoth ioate dihydrobromide
Synonyms L-BMAA hydrochloride
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
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.

Molecular Formula C15H21Br2IN4S
Molecular Weight 576.13200
Exact Mass 573.89000
PSA 89.86000
LogP 5.85400