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5-HT2 antagonist 1

Names

[ CAS No. ]:
191592-09-3

[ Name ]:
5-HT2 antagonist 1

[Synonym ]:
5-{3-[4-(4-Fluorophenyl)-1-piperazinyl]propyl}-8-hydroxy-1-methyl-5,6,7,8-tetrahydropyrrolo[3,2-c]azepin-4(1H)-one
Pyrrolo[3,2-c]azepin-4(1H)-one, 5-[3-[4-(4-fluorophenyl)-1-piperazinyl]propyl]-5,6,7,8-tetrahydro-8-hydroxy-1-methyl-

Biological Activity

[Description]:

5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Cardiovascular Disease

[In Vitro]

5-HT2 antagonist 1 shows 45%, 88%, 93% inhibition of 10 μM erotonin-induced contraction at 10 nM, 100 nM, 1000 nM, respectively, in guinea pig mesentcric artery. 5-HT2 antagonist 1 causes 1% and 10% inhibition of 10 μM norepinephrine-induced contraction at 10 and 100 nM, respectively, in guinea pig aorta[1].

[References]

[1]. Mizuno A, et al. Synthesis and serotonin 2 (5-HT2) receptor antagonist activity of 5-aminoalkyl-substituted pyrrolo[3,2-c]azepines and related compounds. Chem Pharm Bull (Tokyo). 2000 May;48(5):623-35.


[Related Small Molecules]

Isoprenaline hydrochloride | ICI 118,551 (hydrochloride) | Harmine | Phenylephrine hydrochloride | Yohimbine hydrochloride | Pimavanserin | Adrenaline | Ivabradine hydrochloride | Prazosin hydrochloride | Serotonin hydrochloride | Clenbuterol hydrochloride | Sodium Ferulate | Thioridazine hydrochloride | Brexpiprazole | Phentolamine mesilate

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
613.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H29FN4O2

[ Molecular Weight ]:
400.490

[ Flash Point ]:
325.1±31.5 °C

[ Exact Mass ]:
400.227448

[ LogP ]:
0.83

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.629

Related Compounds