CAS 186544-26-3|LY 344864

Introduction：Basic information about CAS 186544-26-3|LY 344864, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. LY 344864 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

Common Name	LY 344864
CAS Number	186544-26-3	Molecular Weight	351.417
Density	1.3±0.1 g/cm3	Boiling Point	471.9±45.0 °C at 760 mmHg
Molecular Formula	C₂₁H₂₂FN₃O	Melting Point	/
MSDS	/	Flash Point	239.2±28.7 °C

Names

Name	N-[(6R)-6-(dimethylamino)-6,7,8,9-tetrahydro-5H-carbazol-3-yl]-4-fluorobenzamide,hydrochloride
Synonym	More Synonyms

LY 344864 BiologicalActivity

Description	LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.IC50 Value: 6 nM (Ki) [1]Target: 5-HT1FLY344864 possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1].in vitro: he 5-HT1A, 5-HT1B and 5-HT1D receptor agonists 8-OH-DPAT (3 microM), CP93129 (3 microM) and L694247 (3 microM), but not the 5-HT1F receptor agonist LY344864 (1 - 3 microM) inhibited evoked IPSCs [2].in vivo: After an intravenous dose of 1 mg/kg, rat plasma LY344864 levels declined with time whereas brain cortex levels remained relatively constant for the first 6 hours after injection. Oral and intravenous LY344864 administration potently inhibited dural protein extravasation caused by electrical stimulation of the trigeminal ganglion in rats [1]. Sumatriptan, zolmitriptan, rizatriptan, and naratriptan all contracted the rabbit saphenous vein from baseline tone, whereas LY344864 in concentrations up to 10(-4) M did not contract the rabbit saphenous vein. Furthermore, vascular contractions to sumatriptan were markedly augmented in the presence of prostaglandin F(2alpha) (PGF(2alpha)). However, even in the presence of PGF(2alpha) (3 x 10(-7) M), LY344864 did not contract the rabbit saphenous vein in concentrations well in excess of its 5-HT(1F) receptor affinity (pK(i) = 8.2) [3].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease
References	[1]. Phebus LA, Johnson KW, Zgombick JM, Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brainpenetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26. [2]. Jeong HJ, Chenu D, Johnson EE, Sumatriptan inhibits synaptic transmission in the rat midbrain periaqueductal grey. Mol Pain. 2008 Nov 11;4:54. [3]. Cohen ML, Schenck K. 5-Hydroxytryptamine(1F) receptors do not participate in vasoconstriction: lack of vasoconstriction to LY344864, a selective serotonin(1F) receptor agonist in rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):935-9.

Description

LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.IC50 Value: 6 nM (Ki) [1]Target: 5-HT1FLY344864 possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1].in vitro: he 5-HT1A, 5-HT1B and 5-HT1D receptor agonists 8-OH-DPAT (3 microM), CP93129 (3 microM) and L694247 (3 microM), but not the 5-HT1F receptor agonist LY344864 (1 - 3 microM) inhibited evoked IPSCs [2].in vivo: After an intravenous dose of 1 mg/kg, rat plasma LY344864 levels declined with time whereas brain cortex levels remained relatively constant for the first 6 hours after injection. Oral and intravenous LY344864 administration potently inhibited dural protein extravasation caused by electrical stimulation of the trigeminal ganglion in rats [1]. Sumatriptan, zolmitriptan, rizatriptan, and naratriptan all contracted the rabbit saphenous vein from baseline tone, whereas LY344864 in concentrations up to 10(-4) M did not contract the rabbit saphenous vein. Furthermore, vascular contractions to sumatriptan were markedly augmented in the presence of prostaglandin F(2alpha) (PGF(2alpha)). However, even in the presence of PGF(2alpha) (3 x 10(-7) M), LY344864 did not contract the rabbit saphenous vein in concentrations well in excess of its 5-HT(1F) receptor affinity (pK(i) = 8.2) [3].

Related Catalog

Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease

References

[1]. Phebus LA, Johnson KW, Zgombick JM, Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brainpenetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26.

[2]. Jeong HJ, Chenu D, Johnson EE, Sumatriptan inhibits synaptic transmission in the rat midbrain periaqueductal grey. Mol Pain. 2008 Nov 11;4:54.

[3]. Cohen ML, Schenck K. 5-Hydroxytryptamine(1F) receptors do not participate in vasoconstriction: lack of vasoconstriction to LY344864, a selective serotonin(1F) receptor agonist in rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):935-9.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	471.9±45.0 °C at 760 mmHg
Molecular Formula	C₂₁H₂₂FN₃O
Molecular Weight	351.417
Flash Point	239.2±28.7 °C
Exact Mass	351.174683
PSA	48.13000
LogP	3.43
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.658
InChIKey	OKUHLSYESBLBCP-PKLMIRHRSA-N
SMILES	CN(C)C1CCc2[nH]c3ccc(NC(=O)c4ccc(F)cc4)cc3c2C1.Cl
Storage condition	2-8℃

Safety Information

HS Code	2933990090

Customs

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide

Benzamide, N-[(3R)-3-(dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluoro-

LY 344864

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