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MedKoo Cat#: 146396 | Name: Zalospirone

Description:

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

Zalospirone is an azapirone-class compound that functions as a selective partial agonist at the 5-HT₁A serotonin receptor. This mechanism is associated with anxiolytic and antidepressant-like effects, as activation of 5-HT₁A receptors can modulate mood and anxiety levels. Clinical trials have demonstrated its potential efficacy in treating anxiety and depression; however, a significant proportion of participants discontinued due to side effects, leading to the cessation of its development .

Chemical Structure

Zalospirone
Zalospirone
CAS#114298-18-9

Theoretical Analysis

MedKoo Cat#: 146396

Name: Zalospirone

CAS#: 114298-18-9

Chemical Formula: C24H29N5O2

Exact Mass: 419.2321

Molecular Weight: 419.53

Elemental Analysis: C, 68.71; H, 6.97; N, 16.69; O, 7.63

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
Zalospirone;
IUPAC/Chemical Name
(3aR,4R,4aR,6aS,7S,7aS)-2-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)-3a,4,4a,6a,7,7a-hexahydro-1H-4,7-ethenocyclobuta[f]isoindole-1,3(2H)-dione
InChi Key
AERLHOTUXIJQFV-RCPZPFRWSA-N
InChi Code
1S/C24H29N5O2/c30-22-20-18-6-7-19(17-5-4-16(17)18)21(20)23(31)29(22)11-2-1-10-27-12-14-28(15-13-27)24-25-8-3-9-26-24/h3-9,16-21H,1-2,10-15H2/t16-,17+,18-,19+,20-,21+
SMILES Code
O=C1[C@H]2[C@H]([C@H]3C=C[C@@H]2[C@@H]4C=C[C@H]34)C(=O)N1CCCCN5CCN(CC5)C6=NC=CC=N6
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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

Preparing Stock Solutions

The following data is based on the product molecular weight 419.53 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
1: Rickels K, Derivan A, Kunz N, Pallay A, Schweizer E. Zalospirone in major depression: a placebo-controlled multicenter study. J Clin Psychopharmacol. 1996 Jun;16(3):212-7. doi: 10.1097/00004714-199606000-00004. PMID: 8784652. 2: Richards JB, Sabol KE, Hand TH, Jolly DC, Marek GJ, Seiden LS. Buspirone, gepirone, ipsapirone, and zalospirone have distinct effects on the differential- reinforcement-of-low-rate 72-s schedule when compared with 5-HTP and diazepam. Psychopharmacology (Berl). 1994 Feb;114(1):39-46. doi: 10.1007/BF02245442. PMID: 7846206. 3: Kishi T, Meltzer HY, Matsuda Y, Iwata N. Azapirone 5-HT1A receptor partial agonist treatment for major depressive disorder: systematic review and meta- analysis. Psychol Med. 2014 Aug;44(11):2255-69. doi: 10.1017/S0033291713002857. Epub 2013 Nov 21. PMID: 24262766. 4: Kelly JP, Wrynn AS, Leonard BE. The olfactory bulbectomized rat as a model of depression: an update. Pharmacol Ther. 1997;74(3):299-316. doi: 10.1016/s0163-7258(97)00004-1. PMID: 9352586. 5: Singh A, Lucki I. Antidepressant-like activity of compounds with varying efficacy at 5-HT1A receptors. Neuropharmacology. 1993 Apr;32(4):331-40. doi: 10.1016/0028-3908(93)90153-t. PMID: 8497336. 6: Newman-Tancredi A, Gavaudan S, Conte C, Chaput C, Touzard M, Verrièle L, Audinot V, Millan MJ. Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol. 1998 Aug 21;355(2-3):245-56. doi: 10.1016/s0014-2999(98)00483-x. PMID: 9760039. 7: Quaglia MG, Farina A, Bossu E, Dell'Aquila C. Analysis of non-benzodiazepinic anxiolytic agents by capillary zone electrophoresis. J Pharm Biomed Anal. 1995 Apr;13(4-5):505-9. doi: 10.1016/0731-7085(95)01340-q. PMID: 9696563. 8: Fujiwara Y, Tomita H, Hikiji M, Kashihara K, Otsuki S, Ohnuki T, Hamagishi Y, Oki T, Sora I, Roeske WR, et al. Characterization of a cloned rat serotonin 5-HT1A receptor expressed in the HeLa cell line. Life Sci. 1993;52(11):949-58. doi: 10.1016/0024-3205(93)90530-g. PMID: 8095315. 9: Hascoët M, Bourin M, Todd KG, Coüetoux du Tertre A. Anti-conflict effect of 5-HT1A agonists in rats: a new model for evaluating anxiolytic-like activity. J Psychopharmacol. 1994 Jan;8(4):227-37. doi: 10.1177/026988119400800406. PMID: 22298629. 10: Schreiber R, Brocco M, Lefèbvre de Ladonchamps B, Monneyron S, Millan MJ. A drug discrimination analysis of the actions of novel serotonin1A receptor ligands in the rat using the 5-HT1A receptor agonist, 8-hydroxy-2-(di-n- propylamino)tetralin. J Pharmacol Exp Ther. 1995 Nov;275(2):822-31. PMID: 7473172.