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
| Molecular Formula | C22H31N3O3 |
| Molecular Weight | 385.4998 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|
| Characterization of alpha1-adrenoceptor subtypes mediating noradrenaline-induced contraction of rat epididymal vas deferens in calcium-free medium. | 1999 |
|
| Molecular cloning and functional expression of the guinea pig alpha(1a)-adrenoceptor. | 2001 Aug 31 |
|
| Alpha1-adrenoceptor subtypes on rat afferent arterioles assessed by radioligand binding and RT-PCR. | 2001 Jul |
|
| Characterization of alpha1-adrenoceptor-mediated contraction in the mouse thoracic aorta. | 2001 Jul 20 |
|
| Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. | 2001 Jun |
|
| Failure of AH11110A to functionally discriminate between alpha(1)-adrenoceptor subtypes A, B and D or between alpha(1)- and alpha(2)-adrenoceptors. | 2001 Mar |
|
| Use of antisense oligonucleotides to verify the role of the alpha(1A)-adrenergic receptor in the contractility of the rat uterus post partum. | 2001 May |
|
| Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien. | 2001 May 7 |
|
| Functional characterization of alpha1-adrenoceptor subtypes in human subcutaneous resistance arteries. | 2001 Nov |
|
| 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 |
|
| alpha(1A)-adrenoceptors mediate sympathetically evoked pupillary dilation in rats. | 2002 Feb |
|
| 5-HT1A receptor-mediated regulation of mitogen-activated protein kinase phosphorylation in rat brain. | 2002 Oct 4 |
|
| Alpha 1-adrenoceptor subtypes mediating noradrenaline-induced contraction of pulmonary artery from pulmonary hypertensive rats. | 2003 Dec 15 |
|
| Cytosolic Ca2+ and phosphoinositide hydrolysis linked to constitutively active alpha 1D-adrenoceptors in vascular smooth muscle. | 2003 Jun |
|
| Effects of castration and of testosterone replacement on alpha(1)-adrenoceptor subtypes in the rat vas deferens. | 2003 Jun 20 |
|
| Functional characterization of alpha-adrenoceptors mediating pupillary dilation in rats. | 2003 Jun 20 |
|
| The hypotensive effect of BMY 7378 involves central 5-HT1A receptor stimulation in the adult but not in the young rat. | 2004 Nov-Dec |
|
| Pharmacological characterization of alpha1-adrenoceptors in mouse isolated femoral small arteries. | 2004 Oct 25 |
|
| Correlation between mRNA levels and functional role of alpha1-adrenoceptor subtypes in arteries: evidence of alpha1L as a functional isoform of the alpha1A-adrenoceptor. | 2005 Nov |
|
| alpha1-Adrenoceptors in proximal segments of tail arteries from control and reserpinised rats. | 2007 Oct |
|
| Noradrenergic vasoconstriction of pig prostatic small arteries. | 2008 Feb |
|
| The alpha1D-adrenergic receptor induces vascular smooth muscle apoptosis via a p53-dependent mechanism. | 2008 Oct |
|
| Smooth muscle alpha1D-adrenoceptors mediate phenylephrine-induced vasoconstriction and increases in endothelial cell Ca2+ in hamster cremaster arterioles. | 2008 Oct |
|
| 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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 18:41:40 GMT 2023
by
admin
on
Fri Dec 15 18:41:40 GMT 2023
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| Record UNII |
08EI0K81OL
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| Record Status |
Validated (UNII)
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| Record Version |
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21102-94-3
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