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Neoplasms

Urogenital Diseases

Small molecule drug

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Disease Domain	Count

Neoplasms	1

Top 5 Drug Type	Count

Small molecule drug	1

Top 5 Target	Count

STAT3 x TRPV1	1

The block of calcium current showed some voltage‐dependence but there was no indication of any selectivity of action for a calcium channel subtype. The characteristics of the blocking action of capsazepine on the residual current of cells which were pretreated with either □Omega;‐conotoxin or nimodipine were similar to control.

The data suggest that capsazepine, in addition to its competitive antagonism of vanilloid receptors, has a non‐specific blocking action on voltage‐activated calcium channels which should be taken into account when interpreting the effects of this substance on intact preparations in vitro or in vivo.

01 Mar 1997·PainQ1 · MEDICINE

Capsaicin and carbon dioxide act by distinct mechanisms on sensory nerve terminals in the cat cornea

Q1 · MEDICINE

Article

Author: Xiaojie Chen ; Carlos Belmonte ; Humphrey P Rang

The discharge of single afferent units recorded from filaments of the mixed ciliary nerve of anaesthetised cats was used to study the effects of CO2, capsaicin and the capsaicin antagonist, capsazepine, on sensory nerve terminals in the cornea. Units were selected on the basis of their sensitivity to CO2 (98.5% applied to the cornea for 30 s in a moist gas stream). Of these units, about 50% (18/38) also responded to capsaicin (0.1 microM applied as droplet and washed off after 20 s), with a discharge of similar magnitude to that produced by CO2. The other CO2-sensitive units (20/38) did not respond to capsaicin. Capsaicin-sensitive units responded more rapidly to CO2 (mean latency to first spike 0.7 +/- 0.2 s) than capsaicin-insensitive units (mean latency to first spike 5.1 +/- 1.2 s). On the basis of their conduction velocity, both the capsaicin-sensitive and the capsaicin-insensitive groups included both A- and C-fibres. Application of capsazepine (10 microM for 5-20 min) to the cornea reversibly blocked the response of the units to capsaicin without affecting responses to CO2. Units that were acutely desensitised by exposure to capsaicin (0.1 microM) for 30 s, during which time the discharge evoked by capsaicin declined to zero, still responded to CO2, though the response was reduced by 44% compared with controls. It is concluded that activation of sensory afferents in the cat cornea by capsaicin and by CO2 appear to involve distinct mechanisms, since: (a) many CO2- sensitive units are not excited by capsaicin; (b) capsazepine selectively blocks excitation by capsaicin without affecting responses to CO2; and (c) desensitisation to capsaicin impairs only partially the responsiveness to CO2.

100 Deals associated with Sandoz Institute for Medical Research

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100 Translational Medicine associated with Sandoz Institute for Medical Research

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Pipeline

Pipeline Snapshot as of 30 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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