Temanogrel free base · Synonyms: APD791

Temanogrel is a highly selective 5-HT2A receptor antagonist.

For research use only. Not for human or veterinary use.

Target 5-HT Receptor

Research area Neurological Disease

Purity >98% Stock Inquire

Data Sheet SDS

Temanogrel structure

CAS No.: 887936-68-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 598.00	BP-02098-500mg	In stock	Get quote
1 g	USD 1,198.00	BP-02098-1g	In stock	Get quote
2 g	USD 1,988.00	BP-02098-2g	In stock	Get quote
5 g	Inquire	BP-02098-5g	In stock	Inquire

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Description

Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.

Biological activity

In Vitro Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC50 of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively)[1]. Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis with an IC50 of 13±7 nM. In Vivo There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is, for mean arterial pressure, P=0.508 between groups, and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel, plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6 and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h and 2.25 h after the start of treatment

Identifiers

SMILES: O=C(C1=CC(OC)=CC=C1)NC2=CC(C3=CC=NN3C)=C(OCCN4CCOCC4)C=C2
InChIKey: ZEOQUKRCASTCFR-UHFFFAOYSA-N

Specifications

MW (average): 436.5035
Formula: C₂₄H₂₈N₄O₄
CAS No.: 887936-68-7
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO

In vitro: DMSO : 100 mg/mL

Documents

References

[1]. Xiong Y, et al. Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis. J Med Chem. 2010 Jun 10;53(11):4412-21.

[2]. Przyklenk K, et al. Targeted inhibition of the serotonin 5HT2A receptor improves coronary patency in an in vivo model of recurrent thrombosis. J Thromb Haemost. 2010 Feb;8(2):331-40.

[3]. Adams JW, et al. APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology. J Pharmacol Exp Ther. 2009 Oct;331(1):96-103.

Same target

Search 5-HT Receptor

Same research area

Search Neurological Disease