Flibanserin

SKU: F0337

Category: API's & Intermediates

Synonyms: 1,3-Dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-2H-benzimidazol-2-one , BIMT 17 , BIMT 17BS; 167933-07-5
CAS-Number: C₂₀H₂₁F₃N₄O
Molecular Formula: 390.40
Molecular Weight

Product Data
Handling
Safety Information
Details

Specifications

Purity: ≥98% (HPLC)
Identity: 1H-NMR
Appearance: White to beige powder

Properties

Melting Point: 160.0°C-162.0°C
Solvents: DMSO (20mg/ml), DMF (20mg/ml), ethanol (10mg/ml)

Handling Advice: Protect from light and moisture.
Use / Stability: Stable for at least 2 years after receipt when stored at +4°C.
Long Term Storage: +4°C
Short Term Storage: +4°C
Shipping: AMBIENT

Transportation: Packing Group III
RIDADR: 2811 6.1
Signal word: Danger
GHS Symbol: GHS06
Precautionary statements: P261-P301 + P310-P305 + P351 + P338
Hazard statements: H301-H315-H319-H335

Description: Flibanserin is a full agonist of the serotonin 5-HT1A receptor and an antagonist of 5-HT2A (Ki=1nm and 49nM, respectively). It also binds to dopamine D4 receptors with Ki values ranging from 4-24 nM, but demonstrates no affinity for the other 5-HT subtypes or other neurotransmitter receptors. Multifunctional serotonergic ligands like flibanserin that can enhance downstream release of dopamine and norepinephrine while concomitantly reducing serotonin release in the brain circuits that mediate symptoms of reduced sexual interest and desire, are being studied clinically for therapeutic potential to improve sexual functioning. Flibanserin was investigated as a novel, non-hormonal treatment for pre-menopausal women with Hypoactive Sexual Desire Disorder (HSDD). Flibanserin was also found to reduce L-DOPA-induced dyskinesia in a model of Parkinson?s Disease.
References: (1) F. Borsini, et al., Naunyn Schmiedebergs Arch. Pharmacol. 352, 276 (1995) , (2) F. Borsini, et al., Naunyn Schmiedebergs Arch. Pharmacol. 352, 283 (1995) , (3) F. Borsini, et al., Psychopharmacology 134, 378 (1997) , (4) A. Scandroglio, et al., Pharmacol. Res. 43, 179 (2001) , (5) F. Borsini, et al., CNS Drug Rev. 8, 117 (2002) (Review) , (6) R.W. Invernizzi, et al., Br. J. Pharmacol. 139, 1281 (2003) , (7) H. Gelez, et al., J. Sex. Med. 10, 1231 (2013) , (8) S.M. Stahl, CNS Spectr. 20, 1 (2015) (Review) , (9) I. Dhanuka & J.A. Simon, Expert Opin. Pharmacother. 16, 2523 (2015) (Review)
InChi Key: PPRRDFIXUUSXRA-UHFFFAOYSA-N
Smiles: O=C1NC2=CC=CC=C2N1CCN3CCN(C4=CC=CC(C(F)(F)F)=C4)CC3

Flibanserin is a full agonist of the serotonin 5-HT1A receptor and an antagonist of 5-HT2A (Ki=1nm and 49nM, respectively). It also binds to dopamine D4 receptors with Ki values ranging from 4-24 nM, but demonstrates no affinity for the other 5-HT subtypes or other neurotransmitter receptors. Multifunctional serotonergic ligands like flibanserin that can enhance downstream release of dopamine and norepinephrine while concomitantly reducing serotonin release in the brain circuits that mediate symptoms of reduced sexual interest and desire, are being studied clinically for therapeutic potential to improve sexual functioning. Flibanserin was investigated as a novel, non-hormonal treatment for pre-menopausal women with Hypoactive Sexual Desire Disorder (HSDD). Flibanserin was also found to reduce L-DOPA-induced dyskinesia in a model of Parkinson?s Disease.

Artikelnummer: F0337 Kategorie: API's & Intermediates

Zusätzliche Information

Zusätzliche Information

Synonyms	1,3-Dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-2H-benzimidazol-2-one, BIMT 17, BIMT 17BS
Purity	≥98% (HPLC)
Appearance	White to beige powder
CAS-Number	167933-07-5
Molecular Formula	C20H21F3N4O
Molecular Weight	390.40
Identity	1H-NMR
Solvents	DMSO (20mg/ml), DMF (20mg/ml), ethanol (10mg/ml)
Melting Point	160.0°C-162.0°C
Smiles	O=C1NC2=CC=CC=C2N1CCN3CCN(C4=CC=CC(C(F)(F)F)=C4)CC3
InChi Key	PPRRDFIXUUSXRA-UHFFFAOYSA-N
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	+4°C
Handling Advice	Protect from light and moisture.
Use / Stability	Stable for at least 2 years after receipt when stored at +4°C.
Hazard statements	H301-H315-H319-H335
Precautionary statements	P261-P301 + P310-P305 + P351 + P338
GHS Symbol	GHS06
Signal word	Danger
RIDADR	2811 6.1
Transportation	Packing Group III
References	(1) F. Borsini, et al., Naunyn Schmiedebergs Arch. Pharmacol. 352, 276 (1995), (2) F. Borsini, et al., Naunyn Schmiedebergs Arch. Pharmacol. 352, 283 (1995), (3) F. Borsini, et al., Psychopharmacology 134, 378 (1997), (4) A. Scandroglio, et al., Pharmacol. Res. 43, 179 (2001), (5) F. Borsini, et al., CNS Drug Rev. 8, 117 (2002) (Review), (6) R.W. Invernizzi, et al., Br. J. Pharmacol. 139, 1281 (2003), (7) H. Gelez, et al., J. Sex. Med. 10, 1231 (2013), (8) S.M. Stahl, CNS Spectr. 20, 1 (2015) (Review), (9) I. Dhanuka & J.A. Simon, Expert Opin. Pharmacother. 16, 2523 (2015) (Review)
Quantity	5 mg, 25 mg, Bulk