86-13-5 Usage
Description
Benztropine, with the chemical formula 3alpha-diphenylmethoxytropane, is a tropane-based dopamine inhibitor used for the symptomatic treatment of Parkinson's disease. It is a combination molecule between a tropane ring, similar to cocaine, and a diphenyl ether from the dialkylpiperazines determined to be a dopamine uptake inhibitor since 1970.
Uses
Benzatropine is used to reduce?extrapyramidal side effects?of?antipsychotic?treatment. Benzatropine is also a second-line drug for the treatment of Parkinson's disease. It improves?tremor, and may alleviate rigidity and?bradykinesia.Benzatropine is also sometimes used for the treatment of?dystonia, a rare disorder that causes abnormal muscle contraction, resulting in twisting postures of limbs, trunk, or face.
Side effects
These are principally anticholinergic:Dry mouth;Blurred vision;Cognitive changes;Drowsiness;Constipation;Urinary retention;Tachycardia;Anorexia;Severe?delirium?and?hallucinations?(in overdose).
Toxicity
The oral LD50 of benztropine is reported to be of 940 mg/kg in rats.In the presence of overdose with benztropine, it has been observed symptoms of circulatory collapse, cardiac arrest, respiratory depression, respiratory arrest, psychosis, shock, coma, seizure, ataxia, combativeness, anhidrosis, hyperthermia, fever, dysphagia, decreased bowel sounds and sluggish pupils.
Definition
ChEBI: Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to re
uce parkinsonism and akathisia side effects of antipsychotic treatments.
Check Digit Verification of cas no
The CAS Registry Mumber 86-13-5 includes 5 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 2 digits, 8 and 6 respectively; the second part has 2 digits, 1 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 86-13:
(4*8)+(3*6)+(2*1)+(1*3)=55
55 % 10 = 5
So 86-13-5 is a valid CAS Registry Number.
InChI:InChI=1/C21H25NO/c1-22-18-12-13-19(22)15-20(14-18)23-21(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18-21H,12-15H2,1H3/t18-,19-/m1/s1
86-13-5Relevant articles and documents
Targeting the FKBP51/GR/Hsp90 Complex to Identify Functionally Relevant Treatments for Depression and PTSD
Sabbagh, Jonathan J.,Cordova, Ricardo A.,Zheng, Dali,Criado-Marrero, Marangelie,Lemus, Andrea,Li, Pengfei,Baker, Jeremy D.,Nordhues, Bryce A.,Darling, April L.,Martinez-Licha, Carlos,Rutz, Daniel A.,Patel, Shreya,Buchner, Johannes,Leahy, James W.,Koren, John,Dickey, Chad A.,Blair, Laura J.
, p. 2288 - 2299 (2018/06/19)
Genetic and epigenetic alterations in FK506-binding protein 5 (FKBP5) have been associated with increased risk for psychiatric disorders, including post-traumatic stress disorder (PTSD). Some of these common variants can increase the expression of FKBP5, the gene that encodes FKBP51. Excess FKBP51 promotes hypothalamic-pituitary-adrenal (HPA) axis dysregulation through altered glucocorticoid receptor (GR) signaling. Thus, we hypothesized that GR activity could be restored by perturbing FKBP51. Here, we screened 1280 pharmacologically active compounds and identified three compounds that rescued FKBP51-mediated suppression of GR activity without directly activating GR. One of the three compounds, benztropine mesylate, disrupted the association of FKBP51 with the GR/Hsp90 complex in vitro. Moreover, we show that removal of FKBP51 from this complex by benztropine restored GR localization in ex vivo brain slices and primary neurons from mice. In conclusion, we have identified a novel disruptor of the FKBP51/GR/Hsp90 complex. Targeting this complex may be a viable approach to developing treatments for disorders related to aberrant FKBP51 expression.
