Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H31N3O3.2ClH |
| Molecular Weight | 458.422 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.COC1=CC=CC=C1N2CCN(CCN3C(=O)CC4(CCCC4)CC3=O)CC2
InChI
InChIKey=NIBOMXUDFLRHRV-UHFFFAOYSA-N
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
| 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 |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| 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 |
|
| Pharmacological characterization of alpha1-adrenoceptor in mouse iliac artery. | 2002 Dec 5 |
|
| 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 |
|
| Serotonergic serotonin (1A) mixed agonists/antagonists elicit large-magnitude phase shifts in hamster circadian wheel-running rhythms. | 2003 |
|
| Interaction between neuropeptide Y Y1 receptors and alpha1B-adrenoceptors in the neurovascular junction of canine splenic arteries. | 2003 Apr 18 |
|
| Alpha 1-adrenoceptor subtypes mediating noradrenaline-induced contraction of pulmonary artery from pulmonary hypertensive rats. | 2003 Dec 15 |
|
| Evidence for the role of alpha1D- and alpha1A-adrenoceptors in contraction of the rat mesenteric artery. | 2003 Feb |
|
| 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 |
|
| Chromatography studies on bio-affinity of nine ligands of alpha1-adrenoceptor to alpha1D subtypes overexpressed in cell membrane. | 2004 Aug |
|
| Evidence that alpha(1B)-adrenoceptors are involved in noradrenaline-induced contractions of rat tail artery. | 2004 Mar 19 |
|
| The hypotensive effect of BMY 7378 involves central 5-HT1A receptor stimulation in the adult but not in the young rat. | 2004 Nov-Dec |
|
| Cloned human 5-HT1A receptor pharmacology determined using agonist binding and measurement of cAMP accumulation. | 2004 Oct |
|
| Pharmacological characterization of alpha1-adrenoceptors in mouse isolated femoral small arteries. | 2004 Oct 25 |
|
| Differential distribution of functional alph}1-adrenergic receptor subtypes along the rat tail artery. | 2005 Aug |
|
| 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 |
|
| Sympathetic neurotransmission in the rat testicular capsule: functional characterization and identification of mRNA encoding alpha1-adrenoceptor subtypes. | 2006 Aug 14 |
|
| Heterodimers of alpha1B- and alpha1D-adrenergic receptors form a single functional entity. | 2006 Jan |
|
| Effects of alpha1D-adrenergic receptors on shedding of biologically active EGF in freshly isolated lacrimal gland epithelial cells. | 2006 Nov |
|
| Selective agonists reveal alpha(1A)- and alpha(1B)-adrenoceptor subtypes in caudal artery of the young rat. | 2006 Oct |
|
| Alpha(1A/L)-adrenoceptors mediate contraction of the circular smooth muscle of the pig urethra. | 2006 Oct |
|
| Identification of alpha-1L and alpha-1A adrenoceptors in human prostate by tissue segment binding. | 2007 Jan |
|
| Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed. | 2007 Jul |
|
| alpha1-Adrenoceptors in proximal segments of tail arteries from control and reserpinised rats. | 2007 Oct |
|
| Different affinities of native alpha1B-adrenoceptors for ketanserin between intact tissue segments and membrane preparations. | 2008 Apr 28 |
|
| 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 |
|
| Mechanical function and gene expression of alpha(1)-adrenoceptor subtypes in dog intravesical ureter. | 2009 Aug |
|
| Adventitia removal does not modify the alphaID-adrenoceptors response in aorta during hypertension and ageing. | 2009 Jul |
|
| Phenylephrine contracts porcine pulmonary veins via alpha(1B)-, alpha(1D)-, and alpha(2)-adrenoceptors. | 2009 Jun 24 |
|
| 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
Sat Dec 16 09:57:48 UTC 2023
by
admin
on
Sat Dec 16 09:57:48 UTC 2023
|
| Record UNII |
KC07KV8T5O
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
DTXSID10175334
Created by
admin on Sat Dec 16 09:57:48 UTC 2023 , Edited by admin on Sat Dec 16 09:57:48 UTC 2023
|
PRIMARY | |||
|
210172
Created by
admin on Sat Dec 16 09:57:48 UTC 2023 , Edited by admin on Sat Dec 16 09:57:48 UTC 2023
|
PRIMARY | |||
|
21102-95-4
Created by
admin on Sat Dec 16 09:57:48 UTC 2023 , Edited by admin on Sat Dec 16 09:57:48 UTC 2023
|
PRIMARY | |||
|
BMY-7378
Created by
admin on Sat Dec 16 09:57:48 UTC 2023 , Edited by admin on Sat Dec 16 09:57:48 UTC 2023
|
PRIMARY | |||
|
KC07KV8T5O
Created by
admin on Sat Dec 16 09:57:48 UTC 2023 , Edited by admin on Sat Dec 16 09:57:48 UTC 2023
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
TARGET -> INHIBITOR |
Binding assay
IC50
|
||
|
|
PARENT -> SALT/SOLVATE |
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
|