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MedKoo Cat#: 598842 | Name: Lidanserin
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Description:

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

Lidanserin is a potential antihypertensive compound which combines vasodilatatory effects due to selective alpha 1-receptor antagonistic action and platelet antiaggregatory, antivasospastic, and vasoprotective properties due to selective 5-HT2-receptor blockade.

Chemical Structure

Lidanserin
Lidanserin
CAS#73725-85-6

Theoretical Analysis

MedKoo Cat#: 598842

Name: Lidanserin

CAS#: 73725-85-6

Chemical Formula: C26H31FN2O4

Exact Mass: 454.2268

Molecular Weight: 454.54

Elemental Analysis: C, 68.70; H, 6.87; F, 4.18; N, 6.16; O, 14.08

Price and Availability

Size Price Availability Quantity
1mg USD 520.00 2 Weeks
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Synonym
Lidanserin; ZK 33839; ZK-33839; ZK33839; Lidanserinum; Lidanserine; Lidanserina;
IUPAC/Chemical Name
4-(3-(3-(4-(4-fluorobenzoyl)piperidin-1-yl)propoxy)-4-methoxyphenyl)pyrrolidin-2-one
InChi Key
JDYWZVJXSMADHP-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H31FN2O4/c1-32-23-8-5-20(21-16-25(30)28-17-21)15-24(23)33-14-2-11-29-12-9-19(10-13-29)26(31)18-3-6-22(27)7-4-18/h3-8,15,19,21H,2,9-14,16-17H2,1H3,(H,28,30)
SMILES Code
O=C1NCC(C2=CC=C(OC)C(OCCCN3CCC(C(C4=CC=C(F)C=C4)=O)CC3)=C2)C1
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
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Lidanserin (ZK-33839) acts as a 5-HT2A and α1-adrenergic receptor antagonist.
In vitro activity:
The pharmacodynamic profile of ZK 33.839 has been investigated under in vitro and in vivo conditions. In human platelets, in rat vascular smooth muscle and in guinea pig tracheal smooth muscle 5-HT-induced proaggregatory and contractile effects were inhibited dose-dependently with IC50-values ranging from 1.85 x 10(-8) mol/l to 9 x 10(-9) mol/l. Reference: Arzneimittelforschung. 1988 Jun;38(6):765-70. https://pubmed.ncbi.nlm.nih.gov/2902861/
In vivo activity:
ZK 33.839 was found to be a potent alpha 1-receptor antagonist, the pA2-value in rat aortic strips determined against phenylephrine was 9.16. ZK 33.839 lowered blood pressure in conscious Dahl-S-rats and in anaesthetized rabbits. Reference: Arzneimittelforschung. 1988 Jun;38(6):765-70. https://pubmed.ncbi.nlm.nih.gov/2902861/
Solvent mg/mL mM comments
Solubility
DMSO 50.0 110.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 454.54 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. Schröder G, Beckmann R, Gerbling KP, Loge O, Maass B, Müller B, Seidelmann D, Schneider HH, Schulz BG, Stürzebecher CS. Pharmacological profile of a new potent 5-hydroxytryptamine (5-HT2) alpha 1-receptor antagonist. Arzneimittelforschung. 1988 Jun;38(6):765-70. PMID: 2902861.
In vitro protocol:
1. Schröder G, Beckmann R, Gerbling KP, Loge O, Maass B, Müller B, Seidelmann D, Schneider HH, Schulz BG, Stürzebecher CS. Pharmacological profile of a new potent 5-hydroxytryptamine (5-HT2) alpha 1-receptor antagonist. Arzneimittelforschung. 1988 Jun;38(6):765-70. PMID: 2902861.
In vivo protocol:
1. Schröder G, Beckmann R, Gerbling KP, Loge O, Maass B, Müller B, Seidelmann D, Schneider HH, Schulz BG, Stürzebecher CS. Pharmacological profile of a new potent 5-hydroxytryptamine (5-HT2) alpha 1-receptor antagonist. Arzneimittelforschung. 1988 Jun;38(6):765-70. PMID: 2902861.
1: İlkaya F, Yüce M, Ağrı AE, Güzel H, Balcı H, Uçar F, Babadağı Z, Müjdeci M, Mutlu E. The combination of agomelatine and ritanserin exerts a synergistic interaction in passive avoidance task. Hum Exp Toxicol. 2015 Aug;34(8):787-95. doi: 10.1177/0960327114559613. Epub 2014 Nov 12. PubMed PMID: 25394903. 2: Ponzoni L, Sala M, Braida D. Ritanserin-sensitive receptors modulate the prosocial and the anxiolytic effect of MDMA derivatives, DOB and PMA, in zebrafish. Behav Brain Res. 2016 Nov 1;314:181-9. doi: 10.1016/j.bbr.2016.08.009. Epub 2016 Aug 6. PubMed PMID: 27506653. 3: Wiesbeck GA, Weijers HG, Chick J, Naranjo CA, Boening J. Ritanserin in relapse prevention in abstinent alcoholics: results from a placebo-controlled double-blind international multicenter trial. Ritanserin in Alcoholism Work Group. Alcohol Clin Exp Res. 1999 Feb;23(2):230-5. PubMed PMID: 10069551. 4: Johnson BA, Jasinski DR, Galloway GP, Kranzler H, Weinreib R, Anton RF, Mason BJ, Bohn MJ, Pettinati HM, Rawson R, Clyde C. Ritanserin in the treatment of alcohol dependence--a multi-center clinical trial. Ritanserin Study Group. Psychopharmacology (Berl). 1996 Nov;128(2):206-15. PubMed PMID: 8956382. 5: Gaikwad U, Parle M, Kumar A, Gaikwad D. Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7. PubMed PMID: 20873421. 6: Meert TF. Ritanserin and alcohol abuse and dependence. Alcohol Alcohol Suppl. 1994;2:523-30. Review. PubMed PMID: 8974378. 7: Naranjo CA, Poulos CX, Lanctôt KL, Bremner KE, Kwok M, Umana M. Ritanserin, a central 5-HT2 antagonist, in heavy social drinkers: desire to drink, alcohol intake and related effects. Addiction. 1995 Jul;90(7):893-905. PubMed PMID: 7663312. 8: Pomier-Layrargues G, Giroux L, Rocheleau B, Huet PM. Combined treatment of portal hypertension with ritanserin and propranolol in conscious and unrestrained cirrhotic rats. Hepatology. 1992 May;15(5):878-82. PubMed PMID: 1568730. 9: Mayer G. Ritanserin improves sleep quality in narcolepsy. Pharmacopsychiatry. 2003 Jul;36(4):150-5. PubMed PMID: 12905101. 10: Trenk D, Seiler KU, Buschmann M, Szathmary S, Benn HP, Jähnchen E. Effect of concomitantly administered cimetidine or ranitidine on the pharmacokinetics of the 5-HT2-receptor antagonist ritanserin. J Clin Pharmacol. 1993 Apr;33(4):330-4. PubMed PMID: 8473547. 11: Wiesel FA, Nordström AL, Farde L, Eriksson B. An open clinical and biochemical study of ritanserin in acute patients with schizophrenia. Psychopharmacology (Berl). 1994 Feb;114(1):31-8. PubMed PMID: 7846205. 12: Wu KM, Hunter TL, Proakis AG. Effects of ritanserin on transmembrane action potentials in canine Purkinje fibers. Proc Soc Exp Biol Med. 1992 Jan;199(1):88-92. PubMed PMID: 1728042. 13: Zhang JJ, Okutani F, Yagi F, Inoue S, Kaba H. Facilitatory effect of ritanserin is mediated by dopamine D(1) receptors on olfactory learning in young rats. Dev Psychobiol. 2000 Dec;37(4):246-52. PubMed PMID: 11084606. 14: Gatch MB, Wallis CJ, Lal H. Effects of ritanserin on ethanol withdrawal-induced anxiety in rats. Alcohol. 2000 May;21(1):11-7. PubMed PMID: 10946153. 15: Gao B, Cutler MG. Effects of acute and subchronic administration of ritanserin on the social behaviour of mice. Neuropharmacology. 1993 Mar;32(3):265-72. PubMed PMID: 8474622. 16: Panocka I, Ciccocioppo R, Polidori C, Romagnoli S, Froldi R, Massi M. Possible mechanism of action for the attenuation of ethanol intake induced by ritanserin in rats. Psychopharmacology (Berl). 1996 Nov;128(2):181-90. PubMed PMID: 8956379. 17: Bersani G, Grispini A, Marini S, Pasini A, Valducci M, Ciani N. 5-HT2 antagonist ritanserin in neuroleptic-induced parkinsonism: a double-blind comparison with orphenadrine and placebo. Clin Neuropharmacol. 1990 Dec;13(6):500-6. PubMed PMID: 2125857. 18: Schrott LM, Sweeney WA, Bodensteiner KE, Sparber SB. Late embryonic ritanserin exposure fails to alter normal responses to immune system stimulation in young chicks. Pharmacol Biochem Behav. 1999 Sep;64(1):81-8. PubMed PMID: 10495001. 19: Timmerman P, Woestenborghs R, Lenoir H, Heykants J. Deuterated ritanserin analysis by gas chromatography/mass spectrometry: a sensitive technique to study human ritanserin pharmacokinetics. Biomed Environ Mass Spectrom. 1989 Jul;18(7):498-502. PubMed PMID: 2505878. 20: Ehrman RN, Robbins SJ, Cornish JW, Childress AR, O'Brien CP. Failure of ritanserin to block cocaine cue reactivity in humans. Drug Alcohol Depend. 1996 Nov;42(3):167-74. PubMed PMID: 8912799.