Pirenperone

Names

[ Name ]:
Pirenperone

[Synonym ]:
4H-Pyrido(1,2-a)pyrimidin-4-one,3-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)-2-methyl
3-<2-(4-(4-fluorobenzoyl)piperidino)-ethyl>-2-methyl-4H-pyrido<1,2-a>-pyrimidin-4-one
1-[2-(2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl)ethyl]-4-(4-fluorobenzoyl)piperidine
Pirenperone
EINECS 278-213-5
Pirenperona [INN-Spanish]
Pirenperonum [INN-Latin]
R-47,465
3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]-ethyl]-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one

Biological Activity

[Description]:

Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[References]

[1]. Krstić MK, et, al. Divergent effects of pirenperone, a 5-HT2 antagonist, on the pressor and tachycardic responses to 5-HT in guinea-pigs. Arch Int Physiol Biochim. 1983 Nov;91(4):345-9.

[2]. Ansseau M, et, al. Pilot study of a specific serotonergic antagonist, pirenperone, in the treatment of anxiety disorders. Acta Psychiatr Belg. Sep-Oct 1983;83(5):517-24.

Chemical & Physical Properties

[ Density]:
1.26g/cm3

[ Boiling Point ]:
556.3ºC at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₄FN₃O₂

[ Molecular Weight ]:
393.45

[ Flash Point ]:
290.2ºC

[ Exact Mass ]:
393.18500

[ PSA ]:
54.68000

[ LogP ]:
3.21730

[ Index of Refraction ]:
1.629

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

5-HT inhibits spontaneous contractility of isolated sheep mesenteric lymphatics via activation of 5-HT(4) receptors.

Microvasc. Res. 60(3) , 261-8, (2000)

Spontaneous isometric contractions were measured in rings of sheep mesenteric lymphatic vessels in vitro. 5-Hydroxytryptamine (5-HT) produced a concentration-dependent decrease in spontaneous contract...

Monoamine systems in the discriminative effects of spiradoline, a kappa-opioid agonist.

Pharmacol. Biochem. Behav. 47(3) , 575-8, (1994)

The results of studies on mice indicate that the antinociceptive effects of kappa-opioid agonists are due, in part, to activation of the 5-HT2 type of serotonin receptor. One objective of this study w...

Visual recognition memory in squirrel monkeys: effects of serotonin antagonists on baseline and hypoxia-induced performance deficits.

Pharmacol. Biochem. Behav. 39(4) , 991-6, (1991)

Cognitive deficits resulting from neuropathological brain changes such as Alzheimer's Disease or normal aging are most likely due to alterations in multiple neurotransmitter systems. While the majorit...