Flibanserin

Orukọ Kemikali:

1- (2- (4- (3- (trifluoromethyl) phenyl) piperazin-1-yl) ethyl) -1H-benzo [d] imidazole-2 (3H) - ọkan hydrochloride.

KỌỌDỌ SMILES:

O=C1NC2=CC=CC=C2N1CCN3CCN(C4=CC=CC(C(F)(F)F)=C4)CC3

Koodu InChi:

InChi=1S/C20H21F3N4O/c21-20(22,23)15-4-3-5-16(14-15)26-11-8-25(9-12-26)10-13-27-18- 7-2-1-6-17 (18)24-19 (27)28/h1-7,14H,8-13H2, (H,24,28)

Bọtini InChi:

PPRRDFIXUUSXRA-UHFFFAOYSA-N

Koko-ọrọ:

Flibanserin, 167933-07-5

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu).

Apejuwe:

Flibanserin jẹ agonist kikun ti olugba 5-HT1A (Ki = 1 nM) ati, pẹlu isunmọ kekere, bi antagonist ti olugba 5-HT2A (Ki = 49 nM) ati antagonist tabi alailagbara apa kan agonist ti olugba D4 ( Ki = 4–24 nM). Pelu isọdọkan ti o tobi pupọ ti flibanserin fun olugba 5-HT1A, ati fun awọn idi ti a ko mọ, flibanserin gba awọn olugba 5-HT1A ati 5-HT2A ni vivo pẹlu awọn ipin kanna. Flibanserin tun ni isunmọ kekere fun olugba 5-HT2B (Ki = 89.3 nM) ati olugba 5-HT2C (Ki = 88.3 nM), mejeeji eyiti o huwa bi antagonist ti. Flibanserin ṣafẹri mu awọn olugba 5-HT1A ṣiṣẹ ni kotesi iwaju, ti n ṣe afihan yiyan agbegbe, ati pe a ti rii lati mu dopamine ati awọn ipele norẹpinẹpirini pọ si ati dinku awọn ipele serotonin ninu kotesi prefrontal eku, awọn iṣe ti a pinnu lati jẹ laja nipasẹ ṣiṣiṣẹ ti 5-HT1A. olugba.[12] Bi iru bẹẹ, a ti ṣe apejuwe flibanserin gẹgẹbi norẹpinẹpirini-dopamine disinhibitor (NDDI). Flibanserin ni a fọwọsi ni Oṣu Kẹjọ ọdun 2015 fun itọju awọn obinrin ti o ṣaju-menopausal ti o ni rudurudu ifẹ ibalopọ hypoactive (HSDD).

Àfojúsùn: 5HT