BMY-7378 HCl | CAS#21102-95-4 | 21102-94-3 | 5-HT1A agonist

BMY-7378 HCl
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522666

CAS#: 21102-95-4 (HCl)

Description: BMY 7378 is an agonist at 5-HT1A receptors mediating hypotension and renal sympatho-inhibition in anaesthetised cats. BMY 7378 is also an alpha (2C)-adrenoceptor antagonist. BMY 7378 is a hypotensive agent in the rat, but that its actions are mediated, in part, by central 5-HT(1A) receptor stimulation in the adult and by a nonserotonergic mechanism in the young rat.

Chemical Structure

BMY-7378 HCl

CAS# 21102-95-4 (HCl)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 522666
Name: BMY-7378 HCl
CAS#: 21102-95-4 (HCl)
Chemical Formula: C22H33Cl2N3O3
Exact Mass: 0.00
Molecular Weight: 458.424
Elemental Analysis: C, 57.64; H, 7.26; Cl, 15.47; N, 9.17; O, 10.47

Price and Availability

Size	Price	Availability
10mg	USD 195	2 Weeks
25mg	USD 350	2 Weeks
50mg	USD 550	2 Weeks
100mg	USD 750	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 21102-94-3 (Free base) 21102-95-4 (HCl)

Synonym: BMY 7378; BMY-7378; BMY7378.

IUPAC/Chemical Name: 8-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-8-azaspiro[4.5]decane-7,9-dione dihydrochloride

InChi Key: NIBOMXUDFLRHRV-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H31N3O3.2ClH/c1-28-19-7-3-2-6-18(19)24-13-10-23(11-14-24)12-15-25-20(26)16-22(17-21(25)27)8-4-5-9-22;;/h2-3,6-7H,4-5,8-17H2,1H3;2*1H

SMILES Code: O=C(N(CCN1CCN(C2=CC=CC=C2OC)CC1)C(C3)=O)CC43CCCC4.[H]Cl.[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, not in water

Shelf Life: >2 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:

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Biological target:	An α2C- and α1D-adrenoceptor antagonist and 5-HT1A partial agonist.
In vitro activity:	In ligand-binding studies, BMY 7378 showed 10-fold selectivity for alpha(2C)-adrenoceptors (pK(i) of 6.54) over other alpha(2)-adrenoceptors. It is concluded that BMY 7378, in addition to alpha(1D)-adrenoceptor selectivity in terms of alpha(1)-adrenoceptors, shows selectivity for alpha(2C)-adrenoceptors in terms of alpha(2)-adrenoceptors. Reference: Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41. https://pubmed.ncbi.nlm.nih.gov/16176444/
In vivo activity:	By 30 weeks of age, SHR (spontaneously hypertensive rats) exhibited significant hypertension and cardiac hypertrophy. BMY 7378 and captopril decreased blood pressure and improved hemodynamic parameters and cardiac function in treated SHR vs. untreated SHR (P < 0.05). Histology showed increased cardiomyocyte size, fibrosis, and left ventricular hypertrophy in SHR hearts. BMY 7378 ameliorated fibrosis and cardiac hypertrophy, but had no effect on cardiomyocyte size in SHR. Effects of BMY 7378 were associated with increased α1D-AR protein expression in SHR. Reference: J Hypertens. 2020 Aug;38(8):1496-1503. https://pubmed.ncbi.nlm.nih.gov/32195823/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	25.0	54.53
	DMF	10.0	21.81
	Ethanol	0.2	0.44
	PBS (pH 7.2)	0.5	1.09

Preparing Stock Solutions

The following data is based on the product molecular weight 458.42 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.

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. Cleary L, Murad K, Bexis S, Docherty JR. The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist. Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41. doi: 10.1111/j.1474-8673.2005.00342.x. PMID: 16176444. 2. Rodríguez JE, Saucedo-Campos AD, Vega AV, Ramírez-Hernández D, Martínez-Aguilar L, Jiménez-Flores JR, Andrade-Jorge E, Estrada-Soto SE, Villalobos-Molina R, Touyz RM, Gallardo-Ortíz IA. The α1D-adrenoreceptor antagonist BMY 7378 reverses cardiac hypertrophy in spontaneously hypertensive rats. J Hypertens. 2020 Aug;38(8):1496-1503. doi: 10.1097/HJH.0000000000002412. PMID: 32195823. 3. Villalobos-Molina R, Gil-Flores M, Gallardo-Ortiz IA, López-Guerrero JJ, Ibarra M. The hypotensive effect of BMY 7378 involves central 5-HT1A receptor stimulation in the adult but not in the young rat. Arch Med Res. 2004 Nov-Dec;35(6):495-8. doi: 10.1016/j.arcmed.2004.11.009. PMID: 15631873.
In vitro protocol:	1. Cleary L, Murad K, Bexis S, Docherty JR. The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist. Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41. doi: 10.1111/j.1474-8673.2005.00342.x. PMID: 16176444.
In vivo protocol:	1. Rodríguez JE, Saucedo-Campos AD, Vega AV, Ramírez-Hernández D, Martínez-Aguilar L, Jiménez-Flores JR, Andrade-Jorge E, Estrada-Soto SE, Villalobos-Molina R, Touyz RM, Gallardo-Ortíz IA. The α1D-adrenoreceptor antagonist BMY 7378 reverses cardiac hypertrophy in spontaneously hypertensive rats. J Hypertens. 2020 Aug;38(8):1496-1503. doi: 10.1097/HJH.0000000000002412. PMID: 32195823. 2. Villalobos-Molina R, Gil-Flores M, Gallardo-Ortiz IA, López-Guerrero JJ, Ibarra M. The hypotensive effect of BMY 7378 involves central 5-HT1A receptor stimulation in the adult but not in the young rat. Arch Med Res. 2004 Nov-Dec;35(6):495-8. doi: 10.1016/j.arcmed.2004.11.009. PMID: 15631873.

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1: Cleary L, Murad K, Bexis S, Docherty JR. The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist. Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41. PubMed PMID: 16176444.

2: Villalobos-Molina R, Gil-Flores M, Gallardo-Ortiz IA, López-Guerrero JJ, Ibarra M. The hypotensive effect of BMY 7378 involves central 5-HT1A receptor stimulation in the adult but not in the young rat. Arch Med Res. 2004 Nov-Dec;35(6):495-8. PubMed PMID: 15631873.

3: Velasco C, Guarneri L, Leonardi A, Testa R. Effects of intravenous and infravesical administration of suramin, terazosin and BMY 7378 on bladder instability in conscious rats with bladder outlet obstruction. BJU Int. 2003 Jul;92(1):131-6. PubMed PMID: 12823397.

4: Villalobos-Molina R, López-Guerrero JJ, Ibarra M. The hypotensive effect of BMY 7378 is antagonized by a silent 5-HT(1A) receptor antagonist: comparison with 8-hydroxy-dipropylamino tetralin. Arch Med Res. 2001 Sep-Oct;32(5):389-93. PubMed PMID: 11578753.

5: Byku M, Gannon RL. Effects of the 5HT1A agonist/antagonist BMY 7378 on light-induced phase advances in hamster circadian activity rhythms during aging. J Biol Rhythms. 2000 Aug;15(4):300-5. PubMed PMID: 10942261.

6: Satoh M, Enomoto K, Takayanagi I, Koike K. Differences of antagonism for a selective alpha1D-adrenoceptor antagonist BMY 7378 in the rabbit thoracic aorta and iliac artery. J Smooth Muscle Res. 1998 Aug;34(4):151-8. PubMed PMID: 10102800.

7: Yang HT, Endoh M. Pharmacological evidence for alpha(1D)-adrenoceptors in the rabbit ventricular myocardium: analysis with BMY 7378. Br J Pharmacol. 1997 Dec;122(8):1541-50. PubMed PMID: 9422797; PubMed Central PMCID: PMC1565100.

8: Goetz AS, King HK, Ward SD, True TA, Rimele TJ, Saussy DL Jr. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1995 Jan 16;272(2-3):R5-6. PubMed PMID: 7713154.

9: Fornal CA, Marrosu F, Metzler CW, Tada K, Jacobs BL. Effects of the putative 5-hydroxytryptamine1A antagonists BMY 7378, NAN 190 and (-)-propranolol on serotonergic dorsal raphe unit activity in behaving cats. J Pharmacol Exp Ther. 1994 Sep;270(3):1359-66. PubMed PMID: 7932190.

10: Barrett JE, Gleeson S. Discriminative stimulus effects of 8-OH-DPAT in pigeons: antagonism studies with the putative 5-HT1A receptor antagonists BMY 7378 and NAN-190. Eur J Pharmacol. 1992 Jul 7;217(2-3):163-71. PubMed PMID: 1425937.

11: Grasby PM, Sharp T, Allen T, Grahame-Smith DG. The putative 5-HT1A antagonist BMY 7378 blocks 8-OH-DPAT-induced changes in local cerebral glucose utilization in the conscious rat. Neuropharmacology. 1992 Jun;31(6):547-51. PubMed PMID: 1407394.

12: Greuel JM, Glaser T. The putative 5-HT1A receptor antagonists NAN-190 and BMY 7378 are partial agonists in the rat dorsal raphe nucleus in vitro. Eur J Pharmacol. 1992 Feb 11;211(2):211-9. PubMed PMID: 1535319.

13: Ahlers ST, Weissman BA, Barrett JE. Antagonism studies with BMY-7378 and NAN-190: effects on 8-hydroxy-2-(di-n-propylamino)tetralin-induced increases in punished responding of pigeons. J Pharmacol Exp Ther. 1992 Feb;260(2):474-81. PubMed PMID: 1531359.

14: Stubbs CM, Connor HE, Feniuk W. BMY 7378 is an agonist at 5-HT1A receptors mediating hypotension and renal sympatho-inhibition in anaesthetised cats. Eur J Pharmacol. 1991 May 2;197(1):113-6. PubMed PMID: 1832639.

15: Sharp T, Backus LI, Hjorth S, Bramwell SR, Grahame-Smith DG. Further investigation of the in vivo pharmacological properties of the putative 5-HT1A antagonist, BMY 7378. Eur J Pharmacol. 1990 Feb 13;176(3):331-40. PubMed PMID: 1970304.

16: Zemlan FP, Zieleniewski-Murphy A, Maureen Murphy R, Behbehani MM. BMY 7378: Partial agonist at spinal cord 5-HT(1A) receptors. Neurochem Int. 1990;16(4):515-22. PubMed PMID: 20504590.

17: Chaput Y, de Montigny C. Effects of the 5-hydroxytryptamine receptor antagonist, BMY 7378, on 5-hydroxytryptamine neurotransmission: electrophysiological studies in the rat central nervous system. J Pharmacol Exp Ther. 1988 Jul;246(1):359-70. PubMed PMID: 2839669.

18: Yocca FD, Hyslop DK, Smith DW, Maayani S. BMY 7378, a buspirone analog with high affinity, selectivity and low intrinsic activity at the 5-HT1A receptor in rat and guinea pig hippocampal membranes. Eur J Pharmacol. 1987 Jun 4;137(2-3):293-4. PubMed PMID: 2886356.

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BMY-7378 HCl featured