Phase I, Double-Blind, Placebo-Controlled, Multiple Ascending Dose, Safety, Tolerability, Pharmacokinetic Study of SRX251 Capsules in Healthy Volunteers

This study is the second study to evaluate SRX251 in healthy volunteers and it represents the first multiple dose study. The primary objective of this study is to evaluate the safety and tolerability of escalating multiple oral doses of SRX251 capsules for 5 days in healthy adult volunteers. Levels of the drug in blood plasma will also be determined.

Start Date01 Sep 2007

Sponsor / Collaborator

Azevan Pharmaceuticals, Inc.

NCT00461370 / CompletedPhase 1

Phase I, Double-Blind, Placebo-Controlled, Ascending, Single-Dose, Safety, Tolerability and Pharmacokinetic Study of SRX251 Capsules in Healthy Female Volunteers

The purpose of this study is to determine the safety of SRX251 when given orally. The amount of SRX251 in the blood will also be measured. Healthy women, ages 18-50 years who have been surgically sterilized by tubal ligation, will be enrolled in this study.

Start Date01 Apr 2007

Sponsor / Collaborator

Azevan Pharmaceuticals, Inc.

100 Clinical Results associated with SRX-251

100 Translational Medicine associated with SRX-251

100 Patents (Medical) associated with SRX-251

Literatures (Medical) associated with SRX-251

01 Dec 2020·Brain Research BulletinQ3 · MEDICINE

Evidence of early vasogenic edema following minor head impact that can be reduced with a vasopressin V1a receptor antagonist

Q3 · MEDICINE

Article

Author: Iriah, Sade ; Simon, Neal S ; Lu, Shi-Fang ; Brownstein, Michael J ; Kulkarni, Praveen ; Ferris, Craig F ; Bhosle, Mansi R

BACKGROUNDDoes minor head impact without signs of structural brain damage cause short-term changes in vasogenic edema as measured by an increase apparent diffusion coefficient (ADC) using diffusion weighted imaging? If so, could the increase in vasogenic edema be treated with a vasopressin V1a receptor antagonist? We hypothesized that SRX251, a highly selective V1a antagonist, would reduce vasogenic edema in response to a single minor head impact.METHODSLightly anesthetized male rats were subjected to a sham procedure or a single hit to the forehead using a closed skull, momentum exchange model. Animals recovered in five min and were injected with saline vehicle (n = 8) or SRX251 (n = 8) at 15 min post head impact and again 7-8 hrs later. At 2 h, 6 h, and 24 h post injury, rats were anesthetized and scanned for increases in ADC, a neurological measure of vasogenic edema. Sham rats (n = 6) were exposed to anesthesia and scanned at all time points but were not hit or treated. Images were registered to and analyzed using a 3D MRI rat atlas providing site-specific data on 150 different brain areas. These brain areas were parsed into 11 major brain regions.RESULTSUntreated rats with brain injury showed a significant increase in global brain vasogenic edema as compared to sham and SRX251 treated rats. Edema peaked at 6 h in injured, untreated rats in three brain regions where changes in ADC were observed, but returned to sham levels by 24 h. There were regional variations in the time course of vasogenic edema and drug efficacy. Edema was significantly reduced in cerebellum and thalamus with SRX251 treatment while the basal ganglia did not show a response to treatment.CONCLUSIONA single minor impact to the forehead causes regional increases in vasogenic edema that peak at 6 h but return to baseline within a day in a subset of brain regions. Treatment with a selective V1a receptor antagonist can reduce much of the edema.

01 Dec 2008·BMC NeuroscienceQ3 · MEDICINE

Imaging the neural circuitry and chemical control of aggressive motivation

Q3 · MEDICINE

ArticleOA

Author: Blanchard, Robert ; Stolberg, Tara ; Simon, Neal G. ; Murugavel, Murali ; Blanchard, D. Caroline ; Brevard, Mathew ; Ferris, Craig F. ; Febo, Marcelo ; Kulkarni, Praveen

BACKGROUNDWith the advent of functional magnetic resonance imaging (fMRI) in awake animals it is possible to resolve patterns of neuronal activity across the entire brain with high spatial and temporal resolution. Synchronized changes in neuronal activity across multiple brain areas can be viewed as functional neuroanatomical circuits coordinating the thoughts, memories and emotions for particular behaviors. To this end, fMRI in conscious rats combined with 3D computational analysis was used to identifying the putative distributed neural circuit involved in aggressive motivation and how this circuit is affected by drugs that block aggressive behavior.RESULTSTo trigger aggressive motivation, male rats were presented with their female cage mate plus a novel male intruder in the bore of the magnet during image acquisition. As expected, brain areas previously identified as critical in the organization and expression of aggressive behavior were activated, e.g., lateral hypothalamus, medial basal amygdala. Unexpected was the intense activation of the forebrain cortex and anterior thalamic nuclei. Oral administration of a selective vasopressin V1a receptor antagonist SRX251 or the selective serotonin reuptake inhibitor fluoxetine, drugs that block aggressive behavior, both caused a general suppression of the distributed neural circuit involved in aggressive motivation. However, the effect of SRX251, but not fluoxetine, was specific to aggression as brain activation in response to a novel sexually receptive female was unaffected.CONCLUSIONThe putative neural circuit of aggressive motivation identified with fMRI includes neural substrates contributing to emotional expression (i.e. cortical and medial amygdala, BNST, lateral hypothalamus), emotional experience (i.e. hippocampus, forebrain cortex, anterior cingulate, retrosplenial cortex) and the anterior thalamic nuclei that bridge the motor and cognitive components of aggressive responding. Drugs that block vasopressin neurotransmission or enhance serotonin activity suppress activity in this putative neural circuit of aggressive motivation, particularly the anterior thalamic nuclei.

100 Deals associated with SRX-251

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Primary dysmenorrhea	Phase 1	US	Azevan Pharmaceuticals, Inc.	01 Apr 2007
Aggression	Phase 1	US	Azevan Pharmaceuticals, Inc.	-

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