Calindol hydrochloride

Names

[ Name ]:
Calindol hydrochloride

[Synonym ]:
Calindol Hydrochloride

Biological Activity

[Description]:

Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> CaSR

[In Vitro]

在 2mM Ca2+ 存在的情况下，Calindol 刺激磷脂酰肌醇 (PI) 在表达大鼠或人 CaSR 的细胞中的 EC50 分别为 1.0 μM 或 0.31 μM[2]。在线肌造影研究中，Calindol (1-10 µM) 抑制 Methoxamine 和 KCl 诱导的预收缩张力，并抑制兔肠系膜动脉中的全细胞电压门控 Ca2+ 通道 (VGCC) 电流[3]。

[References]

[1]. Lionel Kiefer, et al. Design and synthesis of calindol derivatives as potent and selective calcium sensing receptor agonists. Bioorg Med Chem. 2016 Feb 15;24(4):554-69.

[2]. Albane Kessler, et al. N2-benzyl-N1-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamines and conformationally restrained indole analogues: development of calindol as a new calcimimetic acting at the calcium sensing receptor. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3345-9.

[3]. Harry Z E Greenberg, et al. The calcilytics Calhex-231 and NPS 2143 and the calcimimetic Calindol reduce vascular reactivity via inhibition of voltage-gated Ca2+ channels. Eur J Pharmacol. 2016 Nov 15;791:659-668.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₁ClN₂

[ Molecular Weight ]:
336.85800

[ Exact Mass ]:
336.13900

[ PSA ]:
27.82000

[ LogP ]:
6.36480

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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