Cinolazepam |
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| Trade names | Gerodorm 40mg |
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| AHFS/Drugs.com | cinolazepam |
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Dependence liability | High |
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Addiction liability | Medium |
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Routes of administration | Oral |
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| Legal status |
- US: Unscheduled
- EU: Prescription drug
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| Bioavailability | 90–100% |
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| Metabolism | Hepatic |
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| Onset of action | 30 minutes to 1 hour |
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| Elimination half-life | 9 hours |
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| Duration of action | 9 hours |
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| Excretion | Renal |
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(RS)-3-[9-Chloro-6-(2-fluorophenyl)-4-hydroxy-3-oxo-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-2-yl]propanenitrile
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| Formula | C18H13ClFN3O2 |
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| Molar mass | 357.77 g·mol−1 |
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| 3D model (JSmol) | |
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| Chirality | Racemic mixture |
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FC1=CC=CC=C1C2=NC(C(N(CCC#N)C3=C2C=C(C=C3)Cl)=O)O
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InChI=1S/C18H13ClFN3O2/c19-11-6-7-15-13(10-11)16(12-4-1-2-5-14(12)20)22-17(24)18(25)23(15)9-3-8-21/h1-2,4-7,10,17,24H,3,9H2 YKey:XAXMYHMKTCNRRZ-UHFFFAOYSA-N Y
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N Y (what is this?) (verify) |
Cinolazepam[1] (marketed under the brand name Gerodorm)[2] is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.
Due to its strong sedative properties, it is primarily used as a hypnotic.
It was patented in 1978 and came into medical use in 1992.[3] Cinolazepam is mainly used in Romania and Slovakia; it not approved for sale in the United States or Canada.
References
- ^ US Patent 4388313 Novel 3-hydroxy-1,4-benzodiazepine-2-ones and process for the preparation thereof
- ^ Lannacher Romania (1999). "Gerodorm". Produse Gerot inregistrate in Romania (in Romanian). Archived from the original on 11 October 2006. Retrieved 17 August 2006.
- ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 530. ISBN 9783527607495.
External links
Benzodiazepines |
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| 1,4-Benzodiazepines | |
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| 1,5-Benzodiazepines |
- Arfendazam
- Clobazam
- CP-1414S
- Lofendazam
- Triflubazam
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| 2,3-Benzodiazepines* |
- Girisopam
- GYKI-52466
- GYKI-52895
- Nerisopam
- Talampanel
- Tofisopam
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| Triazolobenzodiazepines |
- Adinazolam
- Alprazolam
- Balovaptan*
- Bromazolam
- Clonazolam
- Estazolam
- Fluadinazolam
- Flualprazolam
- Flubromazolam
- Flunitrazolam
- Nitrazolam
- Phenazolam
- Pyrazolam
- Rilmazolam (active metabolite of Rilmazafone)
- Triazolam
|
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| Imidazobenzodiazepines |
- Bretazenil
- Climazolam
- EVT-201
- FG-8205
- Flumazenil
- GL-II-73
- Imidazenil
- 123I-Iomazenil
- L-655,708
- Loprazolam
- Midazolam
- PWZ-029
- Remimazolam
- Ro15-4513
- Ro48-6791
- Ro48-8684
- Ro4938581
- Sarmazenil
- SH-053-R-CH3-2′F
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| Oxazolobenzodiazepines | |
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| Thienodiazepines | |
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| Thienotriazolodiazepines |
- α-Hydroxyetizolam
- Apafant*
- Brotizolam
- Ciclotizolam
- Clotizolam
- Deschloroclotizolam
- Deschloroetizolam
- Etizolam
- Flubrotizolam
- Fluclotizolam
- Fluetizolam
- Israpafant*
- JQ1*
- Metizolam
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| Thienobenzodiazepines* | |
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| Pyridodiazepines | |
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| Pyridotriazolodiazepines | |
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| Pyrazolodiazepines |
- Razobazam*
- Ripazepam
- Zolazepam
- Zomebazam
- Zometapine*
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| Pyrrolodiazepines | |
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| Tetrahydroisoquinobenzodiazepines | |
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| Pyrrolobenzodiazepines* | |
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| Benzodiazepine prodrugs |
- Alprazolam triazolobenzophenone
- Avizafone
- Rilmazafone
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* atypical activity profile (not GABAA receptor ligands) |
Hypnotics/sedatives (N05C) |
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| GABAA | | Alcohols | |
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| Barbiturates | |
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| Benzodiazepines | |
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| Carbamates | |
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| Imidazoles | |
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| Monoureides |
- Acecarbromal
- Apronal (apronalide)
- Bromisoval
- Capuride
- Carbromal
- Ectylurea
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| Neurosteroids | |
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| Nonbenzodiazepines | |
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| Phenols |
- Cipepofol (ciprofol)
- Fospropofol
- Propofol
- Propofol hemisuccinate
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| Piperidinediones | |
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| Quinazolinones |
- Afloqualone
- Cloroqualone
- Diproqualone
- Etaqualone
- Mebroqualone
- Mecloqualone
- Methaqualone
- Methylmethaqualone
- Nitromethaqualone
- SL-164
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| Others | |
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| GABAB | |
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| H1 | | Antihistamines | |
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| Antidepressants |
- Serotonin antagonists and reuptake inhibitors
- Tricyclic antidepressants
- Tetracyclic antidepressants
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| Antipsychotics |
- Typical antipsychotics
- Atypical antipsychotics
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| α2-Adrenergic | |
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| 5-HT2A | | Antidepressants |
- Trazodone
- Tricyclic antidepressants
- Tetracyclic antidepressants
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| Antipsychotics |
- Typical antipsychotics
- Atypical antipsychotics
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| Others | |
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| Melatonin | |
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| Orexin |
- Daridorexant
- Lemborexant
- Suvorexant
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| α2δ VDCC | |
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| Others | |
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GABAA receptor positive modulators |
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| Alcohols | |
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| Barbiturates | |
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| Benzodiazepines | |
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| Carbamates |
- Carisbamate
- Carisoprodol
- Clocental
- Cyclarbamate
- Difebarbamate
- Emylcamate
- Ethinamate
- Febarbamate
- Felbamate
- Hexapropymate
- Hydroxyphenamate
- Lorbamate
- Mebutamate
- Meprobamate
- Nisobamate
- Pentabamate
- Phenprobamate
- Procymate
- Styramate
- Tetrabamate
- Tybamate
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| Flavonoids | |
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| Imidazoles |
- Etomidate
- Metomidate
- Methoxyetomidate
- Propoxate
- Isopropoxate
- Butomidate
- Iso-butomidate
- Sec-butomidate
- CF2-Etomidate
- CF3-Etomidate
- CF3-Propoxate
- Flutomidate
- 2,6-Dichloro-3-fluoroetomidate
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| Kava constituents |
- 10-Methoxyyangonin
- 11-Methoxyyangonin
- 11-Hydroxyyangonin
- Desmethoxyyangonin
- 11-Methoxy-12-hydroxydehydrokavain
- 7,8-Dihydroyangonin
- Kavain
- 5-Hydroxykavain
- 5,6-Dihydroyangonin
- 7,8-Dihydrokavain
- 5,6,7,8-Tetrahydroyangonin
- 5,6-Dehydromethysticin
- Methysticin
- 7,8-Dihydromethysticin
- Yangonin
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| Monoureides |
- Acecarbromal
- Apronal (apronalide)
- Bromisoval
- Carbromal
- Capuride
- Ectylurea
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| Neuroactive steroids | |
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| Nonbenzodiazepines |
- Imidazopyridines: Alpidem
- DS-1
- Necopidem
- Saripidem
- Zolpidem
- Pyrazolopyrimidines: Divaplon
- Fasiplon
- Indiplon
- Lorediplon
- Ocinaplon
- Panadiplon
- Taniplon
- Zaleplon
- Others: Adipiplon
- AXS-17 (BAER-101, AZD-7325)
- CGS-8216
- CGS-9896
- CGS-13767
- CGS-20625
- CL-218,872
- CP-615,003
- CTP-354
- ELB-139
- GBLD-345
- Imepitoin
- JM-1232
- L-838,417
- Lirequinil (Ro41-3696)
- Miltirone (rosmariquinone)
- NS-2664
- NS-2710
- NS-11394
- Pipequaline
- ROD-188
- RWJ-51204
- SB-205,384
- SX-3228
- TGSC01AA
- TP-003
- TPA-023
- TP-13
- U-89843A
- U-90042
- Viqualine
- Y-23684
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| Phenols | |
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| Piperidinediones | |
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| Pyrazolopyridines |
- Cartazolate
- Etazolate
- ICI-190,622
- Tracazolate
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| Quinazolinones |
- Afloqualone
- Cloroqualone
- Diproqualone
- Etaqualone
- Mebroqualone
- Mecloqualone
- Methaqualone
- Methylmethaqualone
- Nitromethaqualone
- SL-164
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| Volatiles/gases | |
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| Others/unsorted |
- 3-Hydroxybutanal
- α-EMTBL
- AA-29504
- Alogabat
- Avermectins (e.g., ivermectin)
- Bromide compounds (e.g., lithium bromide, potassium bromide, sodium bromide)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
- Darigabat
- DEABL
- Deuterated etifoxine
- Dihydroergolines (e.g., dihydroergocryptine, dihydroergosine, dihydroergotamine, ergoloid (dihydroergotoxine))
- DS2
- Efavirenz
- Etazepine
- Etifoxine
- Fenamates (e.g., flufenamic acid, mefenamic acid, niflumic acid, tolfenamic acid)
- Fluoxetine
- Flupirtine
- Hopantenic acid
- KRM-II-81
- Lanthanum
- Lavender oil
- Lignans (e.g., 4-O-methylhonokiol, honokiol, magnolol, obovatol)
- Loreclezole
- Menthyl isovalerate (validolum)
- Monastrol
- Nicotinic acid
- Nicotinamide
- Org 25,435
- Phenytoin
- Propanidid
- Retigabine (ezogabine)
- Safranal
- Seproxetine
- Stiripentol
- Sulfonylalkanes (e.g., sulfonmethane (sulfonal), tetronal, trional)
- Terpenoids (e.g., borneol)
- Topiramate
- Valerian constituents (e.g., isovaleric acid, isovaleramide, valerenic acid, valerenol)
- Unsorted benzodiazepine site positive modulators: α-Pinene
- MRK-409 (MK-0343)
- TCS-1105
- TCS-1205
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See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators |