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MedKoo Cat#: 598567 | Name: Lenperone

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lenperone is an antipsychotic of the butyrophenone class; like other major tranquilizers, it has some alpha-adrenergic blocking action & is antiemetic.

Chemical Structure

Lenperone
Lenperone
CAS#24678-13-5

Theoretical Analysis

MedKoo Cat#: 598567

Name: Lenperone

CAS#: 24678-13-5

Chemical Formula: C22H23F2NO2

Exact Mass: 371.1697

Molecular Weight: 371.43

Elemental Analysis: C, 71.14; H, 6.24; F, 10.23; N, 3.77; O, 8.61

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Related CAS #
24677-86-9 (HCl)
Synonym
Lenperone; Lenperonum; AHR-2277 [as hydrochloride];
IUPAC/Chemical Name
4-(4-(4-fluorobenzoyl)piperidin-1-yl)-1-(4-fluorophenyl)butan-1-one
InChi Key
WCIBOXFOUGQLFC-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H23F2NO2/c23-19-7-3-16(4-8-19)21(26)2-1-13-25-14-11-18(12-15-25)22(27)17-5-9-20(24)10-6-17/h3-10,18H,1-2,11-15H2
SMILES Code
O=C(C1=CC=C(F)C=C1)CCCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Lenperone is an antipsychotic of the butyrophenone class.
In vitro activity:
TBD
In vivo activity:
Before and after 3 wk of acclimation, the monkeys were given a heat-tolerance test in which rectal (Tre) and mean skin (Tsk) temperatures, heart rate, and sweat rate (msw) were monitored during a 90-min exposure to 45 degrees C heat with 24% relative humidity under lenperone (1.0-1.4 mg/kg im) tranquilization. Reference: J Appl Physiol (1985). 1990 Jul;69(1):232-6. https://pubmed.ncbi.nlm.nih.gov/2203723/

Preparing Stock Solutions

The following data is based on the product molecular weight 371.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Sato F, Owen M, Matthes R, Sato K, Gisolfi CV. Functional and morphological changes in the eccrine sweat gland with heat acclimation. J Appl Physiol (1985). 1990 Jul;69(1):232-6. doi: 10.1152/jappl.1990.69.1.232. PMID: 2203723. 2. Owen MD, Matthes RD, Gisolfi CV. Effects of CSF ANG II and AVP on sweating in the heat-stressed patas monkey. J Appl Physiol (1985). 1989 Jul;67(1):134-40. doi: 10.1152/jappl.1989.67.1.134. PMID: 2759937.
In vitro protocol:
TBD
In vivo protocol:
1. Sato F, Owen M, Matthes R, Sato K, Gisolfi CV. Functional and morphological changes in the eccrine sweat gland with heat acclimation. J Appl Physiol (1985). 1990 Jul;69(1):232-6. doi: 10.1152/jappl.1990.69.1.232. PMID: 2203723. 2. Owen MD, Matthes RD, Gisolfi CV. Effects of CSF ANG II and AVP on sweating in the heat-stressed patas monkey. J Appl Physiol (1985). 1989 Jul;67(1):134-40. doi: 10.1152/jappl.1989.67.1.134. PMID: 2759937.
1: Johnson SE, Zelner A, Sherding RG. Effect of lenperone hydrochloride on gastroesophageal sphincter pressure in healthy dogs. Can J Vet Res. 1989 Apr;53(2):248-50. PubMed PMID: 2565757; PubMed Central PMCID: PMC1255555. 2: Mielke DH, Gallant DM, Kessler C, Roniger JJ. Lenperone: a controlled evaluation in chronic schizophrenic patients. Curr Ther Res Clin Exp. 1975 Nov;18(5):636-40. PubMed PMID: 812640. 3: Cloyd GD, Gilbert DL. Dose calibration studies of lenperone, a new tranquilizer for dogs, cats and swine. Vet Med Small Anim Clin. 1973 Apr;68(4):344 passim. PubMed PMID: 4487932. 4: Woggon B, Franke A, Hucker H, Ruether E, Athen D, Angst J, Hippius H. Antipsychotic effects, side effects and effective dosis of the butyrophenone lenperone (AHR 2277). Int Pharmacopsychiatry. 1977;12(2):113-26. PubMed PMID: 561037. 5: Benson GJ, Thurmon JC, Tranquilli WJ, Corbin JE. Intravenous administration of lenperone and glycopyrrolate followed by continuous infusion of sufentanil in dogs: cardiovascular effects. Am J Vet Res. 1987 Sep;48(9):1372-5. PubMed PMID: 2959181. 6: Sathanathan GL, Angrist BM, Phillips N, Gershon S. Assessment of antipsychotic activity of a butyrophenone analogue, lenperone (AHR 2277). Curr Ther Res Clin Exp. 1974 Aug;16(8):844-7. PubMed PMID: 4217252. 7: Osman MA, Pinchbeck FM, Cheng LK, Wright GJ. Determination of lenperone in dog plasma by high-performance liquid chromatography. J Chromatogr. 1985 Dec 13;345(2):430-5. PubMed PMID: 2868021. 8: Fabre LF, Harris RT. Pilot open-label study of lenperone (AHR 2277), a butyrophenone, in anxiety. Curr Ther Res Clin Exp. 1976 Mar;19(3):328-31. PubMed PMID: 817861. 9: Nakra BR, Jones CJ, Majumdar AK, Gaind R. Preliminary evaluation of a new psychotropic drug, lenperone, in the treatment of acute schizophrenia. Curr Med Res Opin. 1977;4(8):529-34. PubMed PMID: 559569. 10: Simpson GM, Varga V. An early clinical trial of lenperone (AHR 2277), a butyrophenone, in chronic schizophrenia. Curr Ther Res Clin Exp. 1974 May;16(5):477-82. PubMed PMID: 4209063. 11: Harris M. Treatment of acute schizophrenia with a new butyrophenone-lenperone. J Clin Pharmacol. 1975 Feb-Mar;15(2-3):187-90. PubMed PMID: 1091666. 12: Chiou GC. Treatment of ocular hypertension and glaucoma with dopamine antagonists. Ophthalmic Res. 1984;16(3):129-34. PubMed PMID: 6147806. 13: Chiou GC, Chen YJ. Improvement of ocular blood flow with dopamine antagonists on ocular-hypertensive rabbit eyes. Zhongguo Yao Li Xue Bao. 1992 Nov;13(6):481-4. PubMed PMID: 1302433. 14: Johnson SE, Zelner A, Sherding RG. Esophageal acid clearance test in healthy dogs. Can J Vet Res. 1989 Apr;53(2):244-7. PubMed PMID: 2713789; PubMed Central PMCID: PMC1255554. 15: Denber HC. Trials with drugs outside the United States. Dis Nerv Syst. 1974 Jul;35(7 Pt. 2):8-9. PubMed PMID: 17894094. 16: Aimoto T, Kaida M, Sato M, Sato M, Kimura R, Murata T. Effects of neuroleptic butyrophenones on pituitary-adrenal activity in rats. J Pharmacobiodyn. 1980 Jan;3(1):46-52. PubMed PMID: 6110713. 17: Chiou GC, Li BH, Chiou FY. Effects of dopamine antagonists injected through vortex veins on intraocular pressure. J Ocul Pharmacol. 1989 Winter;5(4):281-91. PubMed PMID: 2576433. 18: Owen MD, Matthes RD, Gisolfi CV. Effect of cerebrospinal fluid hyperosmolality on sweating in the heat-stressed patas monkey. J Appl Physiol (1985). 1989 Jul;67(1):128-33. PubMed PMID: 2759936. 19: Beaver BV. Animal behavior case of the month. Cat with 7-week history of spraying urine and defecating in house. J Am Vet Med Assoc. 1994 Jan 1;204(1):53-4. PubMed PMID: 7907322. 20: Sato F, Owen M, Matthes R, Sato K, Gisolfi CV. Functional and morphological changes in the eccrine sweat gland with heat acclimation. J Appl Physiol (1985). 1990 Jul;69(1):232-6. PubMed PMID: 2203723.