1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Cipralisant

Cipralisant (Synonyms: GT-2331)

Cat. No.: HY-106993
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Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research.

For research use only. We do not sell to patients.

Cipralisant Chemical Structure

Cipralisant Chemical Structure

CAS No. : 213027-19-1

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Description

Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research[1][2][3][4].

IC50 & Target[3][4]

H3 receptor

9.9 (pKi)

rat H3 receptor

0.47 nM (Ki)

In Vitro

Cipralisant behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant works as a potent full histamine H3 receptor agonist. Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cipralisant (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg[2].
Cipralisant (10 mg/kg; p.o.) completely blocks R-α-methylhistamine-induced drinking[3].
Cipralisant promotes wakefulness in the rat. Cipralisant potently and significantly improves performance in the repeated acquisition model, in line with its high affinity for the rat H3 receptor and good CNS penetration. Cipralisant does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose [2]. Cipralisant behaves as a partial agonist in a rat brain synaptosome model[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SHR pups (35–50 g)[2]
Dosage: 0.3~30 mg/kg
Administration: S.c.
Result: Significantly enhanced performance of the SHR pups in a dose-related manner at 1 mg/kg.
Animal Model: Male Sprague-Dawley rats[3]
Dosage: 10 and 30 mg/kg
Administration: P.o.
Result: Achieved greater brain exposure and water intake was monitored for 60 min after administration.
Molecular Weight

216.32

Formula

C₁₄H₂₀N₂

CAS No.
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