졸피뎀
졸피뎀 · Ivadal · Niotal · Edluar · CS-1159 · ZOLPIDEM · Zoipidem · SL-80.0750
식별자 및 물리적 특성
| CAS No. | 82626-48-0 |
|---|---|
| 분자식 | C19H21N3O |
| 평균 분자량 | 307.4 g/mol |
| 단동위원소 질량 | 307.1684623 g/mol |
| SMILES | Cc1ccc(-c2nc3ccc(C)cn3c2CC(=O)N(C)C)cc1 |
| InChIKey | ZAFYATHCZYHLPB-UHFFFAOYSA-N |
| PubChem CID | 5732 |
| ChEMBL | CHEMBL911 |
| ChEBI | CHEBI:10125 |
| EC No. | 617-367-3 |
| DTXSID | DTXSID7045946 |
| 현지명 | 졸피뎀 |
화학 및 물리적 성질
| XLogP | 2.5 |
|---|---|
| 극성 표면적 | 37.6 |
| 수소 결합 공여자 수 | 0 |
| 수소 결합 수용자 수 | 2 |
| 회전 가능 결합 수 | 3 |
| 무거운 원자 수 | 23 |
| 형식 전하 | 0 |
| 복잡도 | 417 |
| LogP(분배 계수) | 3.02 |
| 용해도 | 2345%(w/v) 수성 2-히드록시프로필-β-시클로덱스트린: 0.3mg/mL |
| 녹는점 | 193-197196 °C189-191°C |
| Physical Description | Solid |
| Dissociation Constants | Strongest basic, 5.65 |
| Kovats Retention Index | 27882908.22797.52814.42756 |
| Collision Cross Section | 177.6 Ų [M+H]+ [CCS Type: DTMethod: single field calibrated]177.2 Ų [M+H]+ [CCS Type: TWMethod: Major Mix IMS/Tof Calibration Kit (Waters)] |
| 밀도 | 1.12±0.1 g/cm3(Predicted) |
| 인화점 | 9℃ |
| 저장 조건 | Store at RT |
| 물리적 상태 | 고체 |
| pKa(산도 계수) | 6.2(at 25℃) |
| 색상 | 하얀색 |
| 용해도 | <10mg/L(상온) |
| 주요 응용 | 임상 시험 |
| InChI | 1S/C19H21N3O/c1-13-5-8-15(9-6-13)19-16(11-18(23)21(3)4)22-12-14(2)7-10-17(22)20-19/h5-10,12H,11H2,1-4H3 |
| InChIKey | ZAFYATHCZYHLPB-UHFFFAOYSA-N |
| SMILES | [n]21c(nc(c2CC(=O)N(C)C)c3ccc(cc3)C)ccc(c1)C |
| NIST | Zolpidem(82626-48-0) |
화학적 성질
Off-White Solid
안전 및 규제
| GHS 분류 | This chemical does not meet GHS hazard criteria for 10% (1 of 10) of reports.WarningH302 (90%): Harmful if swallowed [Warning Acute toxicity, oral]H336 (90%): May cause drowsiness or dizziness [Warning Specific target organ toxicity, single exposureNarcotic effects]H411 (90%): Toxic to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard]P261, P264, P270, P271, P273, P301+P317, P304+P340, P319, P330, P391, P403+P233, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 10 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.Reported as not meeting GHS hazard criteria per 1 of 10 reports by companies.There are 2 notifications provided by 9 of 10 reports by companies with hazard statement code(s).Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. For more detailed information, please visit ECHA C&L website. |
|---|---|
| 규제 정보 | DEA schedule IV controlled substanceStatus: Active Update: 29-05-2018 https://echa.europa.eu/registration-dossier/-/registered-dossier/22051 |
| Hazard Classes and Categories | Acute Tox. 4 (90%)STOT SE 3 (90%)Aquatic Chronic 2 (90%) |
| Treatment | General symptomatic and supportive measures should be used along with immediate gastric lavage where appropriate. Intravenous fluids should be administered as needed. sedative hypnotic effect was shown to be reduced by flumazenil and therefore may be usefulhowever, flumazenil administration may contribute to the appearance of neurological symptoms (convulsions). As in all cases of drug overdose, respiration, pulse, blood pressure, and other appropriate signs should be monitored and general supportive measures employed. Hypotension and CNS depression should be monitored and treated by appropriate medical intervention. Sedating drugs should be withheld following zolpidem overdosage, even if excitation occurs. The value of dialysis in the treatment of overdosage has not been determined, although hemodialysis studies in patients with renal failure receiving therapeutic doses have demonstrated that zolpidem is not dialyzable. (L1712) |
용도
개요
Zolpidem hemitamwe is a non-benzodiazepine hypnotic with specific agonist activity at type 1 benzodiazepine receptors, and is indicated for use in insomnia and other sleep disorders. Structurally zolpidem belongs to a chemically distinct class, thus lacking the side-effects and abuse potential of classical benzodiazepines. It is currently being studied as a pre-operative sedative.
용도
A selective benzodiazepine receptor agonist not related chemically to benzodiazepines
일반 설명
Zolpidem (Ambien, an imidazopyridine) andeszopiclone (Lunesta, a cyclopyrrolone) are nonbenzodiazepinesand have been introduced as short- and moderate-acting hypnotics, respectively. Zolpidem exhibits ahigh selectivity for the α1 subunit of benzodiazepinebindingsite on GABAA receptor complex, whereas eszopicloneis a “superagonist” at BzRs with the subunitcomposition α1β2γ2 and α1β2γ3. Zolpidem has a rapidonset of action of 1.6 hours and good bioavailability(72%), mainly because it is lipophilic and has no ionizablegroups at physiological pH. Food can prolong the time topeak concentration without affecting the half-life probablyfor the same reason. It has short elimination half-life, becauseits aryl methyl groups is extensively α-hydroxylatedto inactive metabolites by CYP3A4 followed by furtheroxidation by aldehyde dehydrogenase to the ionic carboxylicacid. The metabolites are inactive, short-lived, andeliminated in the urine. Its half-life in the elderly or the patientswith liver disease is increased. Therefore, dosingshould be modified in patients with hepatic insufficiencyand the elderly. Because it has longer elimination half-lifethan zaleplon, it may be preferred for sleep maintenance.It was the most commonly prescribed drug for insomniain 2001.