Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H31N3O3 |
| Molecular Weight | 385.4998 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=CC=C1N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2
InChI
InChIKey=AYYCFGDXLUPJAQ-UHFFFAOYSA-N
InChI=1S/C22H31N3O3/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
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/1970304
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/1970304
BMY-7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3. BMY-7378 was at the preclinical stage of development for the treatment of anxiety disorders, but later was discontinued.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. | 1997 |
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| Characterization of alpha1-adrenoceptor-mediated contraction in the mouse thoracic aorta. | 2001 Jul 20 |
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| The hypotensive effect of BMY 7378 is antagonized by a silent 5-HT(1A) receptor antagonist: comparison with 8-hydroxy-dipropylamino tetralin. | 2001 Sep-Oct |
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| alpha(1A)-adrenoceptors mediate sympathetically evoked pupillary dilation in rats. | 2002 Feb |
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| 5-HT1A receptor-mediated regulation of mitogen-activated protein kinase phosphorylation in rat brain. | 2002 Oct 4 |
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| Interaction between neuropeptide Y Y1 receptors and alpha1B-adrenoceptors in the neurovascular junction of canine splenic arteries. | 2003 Apr 18 |
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| Evidence for the role of alpha1D- and alpha1A-adrenoceptors in contraction of the rat mesenteric artery. | 2003 Feb |
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| Cytosolic Ca2+ and phosphoinositide hydrolysis linked to constitutively active alpha 1D-adrenoceptors in vascular smooth muscle. | 2003 Jun |
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| Chromatography studies on bio-affinity of nine ligands of alpha1-adrenoceptor to alpha1D subtypes overexpressed in cell membrane. | 2004 Aug |
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| Cloned human 5-HT1A receptor pharmacology determined using agonist binding and measurement of cAMP accumulation. | 2004 Oct |
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| Effects of alpha1D-adrenergic receptors on shedding of biologically active EGF in freshly isolated lacrimal gland epithelial cells. | 2006 Nov |
|
| Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed. | 2007 Jul |
|
| Inhibitory effect of fentanyl on phenylephrine-induced contraction of the rat aorta. | 2009 Jun 30 |
Sample Use Guides
Rats: BMY-7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats.
Route of Administration:
Other
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08EI0K81OL
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DTXSID70943430
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2419
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21102-94-3
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admin on Fri Dec 15 18:41:40 GMT 2023 , Edited by admin on Fri Dec 15 18:41:40 GMT 2023
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
