BRL-15572 Dihydrochloride - 10mM in DMSO, high purity , CAS No.193611-72-2(DMSO)

Item Number

B408254

• Specifications & Purity: 10mM in DMSO
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

BRL-15572 is a5-HT1Dreceptor antagonist withpKiof 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.
In vitro

BRL-15572 displays high affinity and selectivity for h5-HT_1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT_1D than 5-HT_1B receptors. BRL-15572 binds to h5-HT_1B and h5-HT_1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [³⁵S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT_1B and h5-HT_1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT_1A, 5-HT_1B, 5-HT_1E, 5-HT_1F, 5-HT_2A, 5-HT_2B, 5-HT_2C, 5-HT₆ and 5-HT₇ with pK_i of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT_1D cell line, both BRL-15572 (1 µM) shifts the 5-HT concentration response curve with pK_B of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT_1A and 5-HT_2B receptors. In human atrial appendages, the electrically evoked tritium overflow is inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors). The inhibitory effect of 5-HT on the K⁺-evoked overflow of glutamate is antagonized by the h5-HT_1D receptor ligand BRL-15572. BRL-15572 (1 μM) is unable to modify the effect of 5-HT at the autoreceptor regulating [³H]5-HT release. The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247.

In vivo

In diabetic pithed rats, administration of the selective 5-HT_1D receptor antagonist BRL-15572 (2 mg/kg) does not modify the decreased HR induced by vagal electrical stimulation. The effects of L-694,247 (50 μg/kg), a selective agonist for non-rodent 5-HT_1B and 5-HT_1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572.
Cell Data

cell lines：

Concentrations：0 μM -10 μM

Incubation Time：30 minutes

Powder Purity:≥99%