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MedKoo Cat#: 574373 | Name: MDL-73005EF hydrochloride

Description:

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

MDL 73005EF hydrochloride is a selective 5-HT1A partial agonist.

Chemical Structure

MDL-73005EF hydrochloride
MDL-73005EF hydrochloride
CAS#102908-60-1

Theoretical Analysis

MedKoo Cat#: 574373

Name: MDL-73005EF hydrochloride

CAS#: 102908-60-1

Chemical Formula: C20H27ClN2O4

Exact Mass: 394.1659

Molecular Weight: 394.90

Elemental Analysis: C, 60.83; H, 6.89; Cl, 8.98; N, 7.09; O, 16.21

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No Data
Synonym
MDL-73005EF hydrochloride, MDL 73005EF HCl
IUPAC/Chemical Name
8-[2-(1,4-Benzodioxan-2-ylmethylamino)ethyl]-8-azaspiro[4.5]decane-7,9-dione hydrochloride
InChi Key
UEDYXFOPCMTXEH-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H26N2O4.ClH/c23-18-11-20(7-3-4-8-20)12-19(24)22(18)10-9-21-13-15-14-25-16-5-1-2-6-17(16)26-15;/h1-2,5-6,15,21H,3-4,7-14H2;1H
SMILES Code
O=C(N(CCNCC1OC2=CC=CC=C2OC1)C(C3)=O)CC43CCCC4.[H]Cl
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:
MDL 73005EF hydrochloride is a potent and selective 5-HT1A receptor antagonist.
In vitro activity:
The effect of a novel ligand for the 5-HT1A receptor subtype, MDL 73005EF, on the firing rate of serotonergic dorsal raphe neurons was assessed in rat midbrain slices maintained in vitro. Superfusion with MDL 73005EF inhibited neuronal firing in a concentration-dependent manner. Pretreatment with (-)-propranolol (1 microM), a mixed 5-HT1A/B receptor antagonist, blocked by 50% the inhibition of unit activity elicited by MDL 73005EF. Taken together, these data suggest that MDL 73005EF is an agonist at the somatodendritic autoreceptor on dorsal raphe neurons, a 5-HT1A receptor which regulates in part the pacemaker activity of these cells. Reference: Eur J Pharmacol. 1991 Aug 29;201(2-3):163-9. https://pubmed.ncbi.nlm.nih.gov/1839146/
In vivo activity:
The effects of pretreatment with the potent and selective 5-HT1A receptor ligand, MDL 73005EF, on the cardiovascular responses to administration of the 5-HT1A receptor agonists, 8-hydroxy-2-(di-n- propylamino)tetralin (8-OH-DPAT), flesinoxan and 5-methylurapidil were studied in conscious spontaneously hypertensive rats (SHR) and compared with those of putative 5-HT1A receptor antagonists. Pretreatment with doses of 1 or 3 mg/kg MDL 73005EF significantly inhibited the hypotensive and bradycardiac effects of 8-OH-DPAT (0.03-1 mg/kg). Pretreatment with 1 mg/kg MDL 73005EF similarly reduced the hypotensive actions of flesinoxan (0.3-1 mg/kg) and 5-methylurapidil (0.1 mg/kg). Reference: Eur J Pharmacol. 1992 Nov 17;223(2-3):133-41. https://pubmed.ncbi.nlm.nih.gov/1362161/

Preparing Stock Solutions

The following data is based on the product molecular weight 394.90 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. Sprouse JS. Inhibition of dorsal raphe cell firing by MDL 73005EF, a novel 5-HT1A receptor ligand. Eur J Pharmacol. 1991 Aug 29;201(2-3):163-9. doi: 10.1016/0014-2999(91)90340-v. PMID: 1839146. 2. Kehne JH, McCloskey TC, Baron BM, Chi EM, Harrison BL, Whitten JP, Palfreyman MG. NMDA receptor complex antagonists have potential anxiolytic effects as measured with separation-induced ultrasonic vocalizations. Eur J Pharmacol. 1991 Feb 14;193(3):283-92. doi: 10.1016/0014-2999(91)90141-c. PMID: 1675993. 3. Buisson-Defferier S, Van den Buuse M. Cardiovascular effects of the 5-HT1A receptor ligand, MDL 73005EF, in conscious spontaneously hypertensive rats. Eur J Pharmacol. 1992 Nov 17;223(2-3):133-41. doi: 10.1016/0014-2999(92)94831-f. PMID: 1362161. 4. Van den Hooff P, Galvan M. Electrophysiology of the 5-HT1A ligand MDL 73005EF in the rat hippocampal slice. Eur J Pharmacol. 1991 Apr 24;196(3):291-8. doi: 10.1016/0014-2999(91)90442-s. PMID: 1893914.
In vitro protocol:
1. Sprouse JS. Inhibition of dorsal raphe cell firing by MDL 73005EF, a novel 5-HT1A receptor ligand. Eur J Pharmacol. 1991 Aug 29;201(2-3):163-9. doi: 10.1016/0014-2999(91)90340-v. PMID: 1839146. 2. Kehne JH, McCloskey TC, Baron BM, Chi EM, Harrison BL, Whitten JP, Palfreyman MG. NMDA receptor complex antagonists have potential anxiolytic effects as measured with separation-induced ultrasonic vocalizations. Eur J Pharmacol. 1991 Feb 14;193(3):283-92. doi: 10.1016/0014-2999(91)90141-c. PMID: 1675993.
In vivo protocol:
1. Buisson-Defferier S, Van den Buuse M. Cardiovascular effects of the 5-HT1A receptor ligand, MDL 73005EF, in conscious spontaneously hypertensive rats. Eur J Pharmacol. 1992 Nov 17;223(2-3):133-41. doi: 10.1016/0014-2999(92)94831-f. PMID: 1362161. 2. Van den Hooff P, Galvan M. Electrophysiology of the 5-HT1A ligand MDL 73005EF in the rat hippocampal slice. Eur J Pharmacol. 1991 Apr 24;196(3):291-8. doi: 10.1016/0014-2999(91)90442-s. PMID: 1893914.
1. Buisson Defferier and Van den Buuse (1992) Cardiovascular effects of the 5-HT1A receptor ligand, MDL 73005EF, in conscious hypertensive rats. Eur.J.Pharmacol. 223 133 PMID: 1362161 2. Gartside et al (1990) Effects of MDL 73005EF on central pre-and-postsynaptic 5HT1A receptor function in the rat in vivo. Eur.J.Pharmacol. 191 391 PMID: 1964908 3. Van der Hooff and Galvan (1991) Electrophysiology of the 5-HT1A ligand MDL 73005EF in the rat hippocampal slice. Eur.J.Pharmacol. 196 291 PMID: 1893914