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Quinupramine, キヌプラミン

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Quinupramine

Quinupramine

キヌプラミン

  • 5-(1-azabicyclo[2.2.2]oct-3-yl)-10,11-dihydro-5H-dibenz[b,f]azepine
  • Formula:C21H24N2
  • MW:304.44 g/mol
  • CAS:31721-17-2
Quinupramine
CAS Registry Number: 31721-17-2
CAS Name: 5-(1-Azabicyclo[2.2.2]oct-3-yl)-10,11-dihydro-5H-dibenz[b,f]azepine
Additional Names: 10,11-dihydro-5-(3-quinuclidinyl)-5H-dibenz[b,f]azepine
Manufacturers’ Codes: LM-208
Trademarks: Kinupril (Bellon); Kevopril (Rhone-Poulenc)
Molecular Formula: C21H24N2
Molecular Weight: 304.43
Percent Composition: C 82.85%, H 7.95%, N 9.20%
Literature References: Analog of imipramine, q.v. Prepn: C. Gueremy, P. C. Wirth, DE 2030492 (1971 to Sogeras), C.A. 74,141581e (1971). Animal studies: W. Van Dorsser, A. Dresse, Arch. Int. Pharmacodyn. Ther. 208, 373 (1974); eidem, ibid. 220, 164 (1976). Clinical study: R. Volmat et al., Clin. Neurol. Psychiat. 239, 445 (1978).
Properties: Crystals, mp 150°.
Melting point: mp 150°
Therap-Cat: Antidepressant.
Keywords: Antidepressant; Tricyclics.

Quinupramine (brand names KevoprilKinuprilAdeprimQuinuprine) is a tricyclic antidepressant (TCA) used in Europe for the treatment of depression.[1][2]

Pharmacologically, quinupramine acts in vitro as a strong muscarinic acetylcholine receptor antagonist (anticholinergic) and H1 receptorantagonist (antihistamine), moderate 5-HT2 receptor antagonist, and weak serotonin and norepinephrine reuptake inhibitor.[3] It has negligible affinity for the α1-adrenergicα2-adrenergicβ-adrenergic, or D2 receptor.[3]

Clinically, quinupramine is reported to be stimulating similarly to imipraminedesipramine, and demexiptiline.[4] It can be inferred that its in vivo metabolites may have stronger effects on the reuptake of norepinephrine and/or serotonin than quinupramine itself

SYN

References

  1. ^ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. p. 908. ISBN 3-88763-075-0.
  2. ^ José Miguel Vela; Helmut Buschmann; Jörg Holenz; Antonio Párraga; Antoni Torrens (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH. p. 248. ISBN 978-3-527-31058-6.
  3. Jump up to:a b Sakamoto H, Yokoyama N, Kohno S, Ohata K (December 1984). “Receptor binding profile of quinupramine, a new tricyclic antidepressant”. Japanese Journal of Pharmacology36 (4): 455–60. doi:10.1254/jjp.36.455PMID 6098759.
  4. ^ Kent, Angela; M. Billiard (2003). Sleep: physiology, investigations, and medicine. New York: Kluwer Academic/Plenum. p. 233. ISBN 0-306-47406-9.
    • DOS 2 030 492 (Sogeras; appl. 20.6.1970; GB-prior. 20.6.1969).
    • GB 1 252 320 (Sogeras; valid from 29.5.1970; prior. 20.6.1969).
Quinupramine
Quinupramine.svg
Clinical data
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Elimination half-life 33 hours
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ECHA InfoCard 100.046.149 Edit this at Wikidata
Chemical and physical data
Formula C21H24N2
Molar mass 304.43 g/mol g·mol−1

//////////////Quinupramine, キヌプラミン

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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 year tenure till date Dec 2017, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 50 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 19 lakh plus views on New Drug Approvals Blog in 216 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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